Artykuły w czasopismach: „Pyrimidines”

1

Nwachukwu, Chideraa I., Leanna J. Patton, Nathan P. Bowling i Eric Bosch. "Ditopic halogen bonding with bipyrimidines and activated pyrimidines". Acta Crystallographica Section C Structural Chemistry 76, nr 5 (20.04.2020): 458–67. http://dx.doi.org/10.1107/s2053229620005082.

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The potential of pyrimidines to serve as ditopic halogen-bond acceptors is explored. The halogen-bonded cocrystals formed from solutions of either 5,5′-bipyrimidine (C8H6N4) or 1,2-bis(pyrimidin-5-yl)ethyne (C10H6N4) and 2 molar equivalents of 1,3-diiodotetrafluorobenzene (C6F4I2) have a 1:1 composition. Each pyrimidine moiety acts as a single halogen-bond acceptor and the bipyrimidines act as ditopic halogen-bond acceptors. In contrast, the activated pyrimidines 2- and 5-{[4-(dimethylamino)phenyl]ethynyl}pyrimidine (C14H13N3) are ditopic halogen-bond acceptors, and 1:1 halogen-bonded cocrystals are formed from 1:1 mixtures of each of the activated pyrimidines and either 1,2- or 1,3-diiodotetrafluorobenzene. A 1:1 cocrystal was also formed between 2-{[4-(dimethylamino)phenyl]ethynyl}pyrimidine and 1,4-diiodotetrafluorobenzene, while a 2:1 cocrystal was formed between 5-{[4-(dimethylamino)phenyl]ethynyl}pyrimidine and 1,4-diiodotetrafluorobenzene.

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Verma, Vishal, Chandra Prakash Joshi, Alka Agarwal, Sakshi Soni i Udichi Kataria. "A Review on Pharmacological Aspects of Pyrimidine Derivatives". Journal of Drug Delivery and Therapeutics 10, nr 5 (15.09.2020): 358–61. http://dx.doi.org/10.22270/jddt.v10i5.4295.

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Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. One of the three diazines (six-membered heterocyclics with two nitrogen atoms in the ring), it has the nitrogens at positions 1 and 3 in the ring. Pyrimidines are typically synthesized by the “Principal Synthesis” involving cyclization of beta-dicarbonyl compounds with N-C-N compounds. Reaction of the former with amidines to give 2-substituted pyrimidines, with urea to give 2-pyrimidiones, and guanidines to give 2-aminopyrimidines are typical. Pyrimidines can be prepared via the biginelli reaction. Many other methods rely on condensation of carbonyls with diamines for instance the synthesis of 2-Thio-6-methyluracil from thiouria and ethyl acetoacetate or the synthesis of 4-methylpyrimidine with 4, 4-dimethoxy-2-butanone and formamide. Pyrimidine derivatives show antimicrobial activity, anticancer activity, anti-inflammatory activity, antidiabetic, and analgesic activity.1. Keywords: Pyrimidine derivatives, Synthesis, derivatives and pharmacological activities.

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Borrell, José I., Jordi Teixidó, Blanca Martínez-Teipel, Blanca Serra, Josep Lluís Matallana, Marta Costa i Xavier Batllori. "An Unequivocal Synthesis of 4-Amino-1,5,6,8-tetrahydropyrido[2,3-d]pyrimidine-2,7-diones and 2-Amino-3,5,6,8-tetrahydropyrido[2,3-d]pyrimidine-4,7-diones". Collection of Czechoslovak Chemical Communications 61, nr 6 (1996): 901–9. http://dx.doi.org/10.1135/cccc19960901.

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An unequivocal set of procedures for the synthesis of 4-amino-1,5,6,8-tetrahydropyrido[2,3-d]pyrimidine-2,7-diones (7) and 2-amino-3,5,6,8-tetrahydropyrido[2,3-d]pyrimidine-4,7-diones (8), in a maximum of four steps from an α,β-unsaturated ester 1, is reported. Thus, the acid hydrolysis of the 2,4-diaminopyrido[2,3-d]pyrimidines 3 yields the 4-amino-2-oxopyrido[2,3-d]pyrimidines 7 while the cyclization of the Michael adducts 9 (formed by reaction of 1 and methyl cyanoacetate) with guanidine affords the corresponding 2-amino-4-oxopyrido[2,3-d]pyrimidines 8. Both isomers were also obtained by hydrolysis of the 4-amino-2-bromo- and 2-amino-4-bromo-5,6-dihydropyrido[2,3-d]pyrimidin-7(8H)-ones 5 and 6, respectively.

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Mohammed, F. K., i M. G. Badrey. "Synthesis of Pyrimidines and Heteroannulated Pyrimidine Ring Systems". Journal of the Korean Chemical Society 55, nr 2 (20.04.2011): 218–29. http://dx.doi.org/10.5012/jkcs.2011.55.2.218.

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Ogurtsov, Vladimir A., i Oleg A. Rakitin. "6-(Chloromethyl)-N,1-dimethyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine". Molbank 2021, nr 4 (1.11.2021): M1294. http://dx.doi.org/10.3390/m1294.

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Functionally 4,6-disubstituted 1H-pyrazolo[3,4-d]pyrimidines are important compounds with various pharmacological activities. 1-Substituted 4-chloro-6-(chloromethyl)-1H-pyrazolo[3,4-d]pyrimidines are practically unexplored derivatives in this series. In this paper, it was shown that the nucleophilic substitution of 4-Chloro-6-(chloromethyl)-1-methyl-1H-pyrazolo[3,4-d]pyrimidine with methylamine produced selectively 4-substituted product, 6-(chloromethyl)-N,1-dimethyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine. The structure of the synthesized compound was established by elemental analysis, high resolution mass-spectrometry, 1H, 13C-NMR, and IR spectroscopy, mass-spectrometry, and X-ray analysis.

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6

Hossain, M. I., i M. M. H. Bhuiyan. "Synthesis and Antimicrobial Activities of Some New Thieno and Furopyrimidine Derivatives". Journal of Scientific Research 1, nr 2 (23.04.2009): 317–25. http://dx.doi.org/10.3329/jsr.v1i2.2299.

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Fused pyrimidines, 8,9-dimethyl[1,2,4]triazolo[4,3-c]thieno[3,2-e]pyrimidine 5, 3,8,9-trimethyl[1,2,4]triazolo[4,3-c]thieno[3,2-e]pyrimidine 6, 4-benzylidinehydrazono-5,6 dimethylthieno[2,3-d]pyrimidine 7, 4-[4/-hydroxybenzylidine]hydrazono-5,6-dimethylthi-eno[2,3-d]pyrimidine 8, 4-[4/-tolylidin]hydrazono-5,6-dimethylthieno[2,3-d]pyrimidine 9, 4-[4/-nitrobenzylidine]hydrazono-5-ethyl-6-methylthieno[2,3-d]pyrimidine 10 and 4-[4/-chlorobenzylidine]hydrazono-5-ethyl-6-methylthieno[2,3-d]pyrimidine 11 are prepared in good yield by an initial treatment of 2-amino-4,5-dimethylthiophene-3-carbonitrile 1 with formic acid, affording 5,6-dimethylthieno[2,3-d]pyrimidin-4(3H)-one 2, which is chlorinated with thionyl chloride and then hydrazinated with hydrazine hydrate. Finally hydrazino compound 4 is reacted with formic acid, acetic anhydrate, benzaldehyde, p-hydroxybenzaldehyde, p-toluayldehyde, p-nitrobenzaldehyde and p-chlorobenzaldehyde to give thienotriazolopyrimidines 5-6 and thienopyrimidines 7-11 respectively. All the compounds have been screened for their antimicrobial activity. Keywords: Fused pyrimidines; Hydrazino compound; Thienotriazolopyrmidines; Thienopyrimidines; Antimicrobial activity.© 2009 JSR Publications. ISSN: 2070-0237 (Print); 2070-0245 (Online). All rights reserved.DOI: 10.3329/jsr.v1i2.2299

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7

Solomyannyi, Roman, Sergii Slivchuk, Donald Smee, Jung-ae Choi, Eduard Rusanov, Victor Zhirnov i Volodymyr Brovarets. "In vitro Activity of the Novel Pyrimidines and Their Condensed Derivatives Against Poliovirus". Current Bioactive Compounds 15, nr 5 (3.01.2019): 582–91. http://dx.doi.org/10.2174/1573407214666180720120509.

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Background: Substituted pyrimidine derivatives (non-nucleoside) are found to be associated with various biological activities. The various substituted pyrimidines are also having significant in vitro activity against different DNA and RNA viruses. The present study focuses on the anti-PV activity of new pyrimidines and their condensed derivatives. Methods: A series of novel pyrimidines and their condensed derivatives were synthesized and their structures were confirmed by spectral data. Their antiviral activities against poliovirus type 3 (PV-3) were evaluated in vitro. In cell culture, morphological changes observed in cells infected with polioviruses, including cell rounding and detachment from the substrate, are generally termed cytopathic effects (CPE). The effects of synthetic pyrimidines on PV amplification in a culture of the heteroploid cell line, Vero 76 (African green monkey kidney cells) were investigated. Results: Bioassays in vitro showed that one of seven synthesized compounds, 7-(Benzenesulfonyl)-5- benzyl-N-(prop-2-en-1-yl)-5H-pyrrolo[3,2-d]pyrimidin-4-amine, has potent antiviral activity against PV-3 (EC50 = 0.75 μM). The selectivity index of this compound is similar to that of pirodavir. Conclusion: The need for antiviral agents to treat PV-associated diseases remains great, but few options currently exist. Here we show that substituted pyrimidine derivatives are a promising structure class of chemical compounds for the development of antiviral drugs against PV infections.

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8

Sirakanyan, Spinelli, Geronikaki, Hakobyan, Sahakyan, Arabyan, Zakaryan i in. "Synthesis, Antitumor Activity, and Docking Analysis of New Pyrido[3’,2’:4,5]furo(thieno)[3,2-d]pyrimidin-8-amines". Molecules 24, nr 21 (31.10.2019): 3952. http://dx.doi.org/10.3390/molecules24213952.

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Continuing our research in the field of new heterocyclic compounds, herein we report on the synthesis and antitumor activity of new amino derivatives of pyrido[3’,2’:4,5](furo)thieno[3,2-d]pyrimidines as well as of two new heterocyclic systems: furo[2–e]imidazo[1,2-c]pyrimidine and furo[2,3-e]pyrimido[1,2-c]pyrimidine. Thus, by refluxing the 8-chloro derivatives of pyrido[3’,2’:4,5]thieno(furo)[3,2-d]pyrimidines with various amines, the relevant pyrido[3’,2’:4,5]thieno(furo)[3,2-d]pyrimidin-8-amines were obtained. Further, the cyclization of some amines under the action of phosphorus oxychloride led to the formation of new heterorings: imidazo[1,2-c]pyrimidine and pyrimido[1,2-c]pyrimidine. The possible antitumor activity of the newly synthesized compounds was evaluated in vitro. The biological tests evidenced that some of them showed pronounced antitumor activity. A study of the structure–activity relationships revealed that the compound activity depended mostly on the nature of the amine fragments. A docking analysis was also performed for the most active compounds.

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9

Behera, Manoranjan, M. Sambaiah, Poosa Mallesham, K. Shiva Kumar, Yamini Bobde, Prasanta Hota, Satyanarayana Yennam i Balaram Ghosh. "Tandem Schiff-Base Formation/Heterocyclization: An Approach to the Synthesis of Fused Pyrazolo–Pyrimidine/Isoxazolo-Pyrimidine Hybrids". Synlett 30, nr 05 (5.02.2019): 586–92. http://dx.doi.org/10.1055/s-0037-1612081.

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A new synthesis of pyrazolo[4,3-d]pyrimidines and isoxazolo[4,5-d]pyrimidines is described. Key steps in the synthesis involve Stille coupling of 4,6-dichloro-2-phenyl-pyrimidine with tributyl(1-ethoxyvinyl)stannane and tandem Schiff-base formation/heterocyclization of 2,6-di-aryl-5-fluoro-4-acetylpyrimidine with hydrazines or hydroxylamine to give pyrazolo[4,3-d]pyrimidines and isoxazolo[4,5-d]pyrimidines, respectively. The position of the fluoro group in the pyrimidine ring is important for the success of heterocylization reaction.

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10

Gallagher, P. E., i N. J. Duker. "Detection of UV purine photoproducts in a defined sequence of human DNA". Molecular and Cellular Biology 6, nr 2 (luty 1986): 707–9. http://dx.doi.org/10.1128/mcb.6.2.707-709.1986.

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The UV-irradiated, 3'-end-labeled, 92-base-pair terminus of the human alphoid sequence was incubated with purified endonuclease v. Previously unreported photoproducts were incised at purine loci. These were not pyrimidine photodimers, 6-4'-(pyrimidin-2'-one)-pyrimidines, base loss sites, or ring-opened purines. Therefore, purine-containing photoproducts, possibly dimers, were incised by the enzyme preparation.

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11

Gallagher, P. E., i N. J. Duker. "Detection of UV purine photoproducts in a defined sequence of human DNA." Molecular and Cellular Biology 6, nr 2 (luty 1986): 707–9. http://dx.doi.org/10.1128/mcb.6.2.707.

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The UV-irradiated, 3'-end-labeled, 92-base-pair terminus of the human alphoid sequence was incubated with purified endonuclease v. Previously unreported photoproducts were incised at purine loci. These were not pyrimidine photodimers, 6-4'-(pyrimidin-2'-one)-pyrimidines, base loss sites, or ring-opened purines. Therefore, purine-containing photoproducts, possibly dimers, were incised by the enzyme preparation.

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12

Nerkar, A. G., S. A. Ghone i A. K. Thaker. "In SilicoScreening of the Library of Pyrimidine Derivatives as Thymidylate Synthase Inhibitors for Anticancer Activity". E-Journal of Chemistry 6, nr 3 (2009): 665–72. http://dx.doi.org/10.1155/2009/352717.

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We here report the virtual screening of several series of pyrimidine derivatives forin silicoThymidylate Synthase (TS) inhibition to arrive at possible potential inhibitors of TS with acceptable pharmacokinetic or ADME (Absorption, Distribution, Metabolism and Excretion) properties. Library of the molecules was constructed based upon structural modifications of pyrimidines nucleus. Structural modifications in descending order were performed for the series of pyrimidines,vizfrom pyrimidines with five membered heterocyclic ring to pyrimidines with four membered heterocyclic ring to simple pyrimindine carboxylates in an order to arrive at pyrimidines with better inhibition scores (G-Scores) as compared with Raltitrexed (RTX) and active metabolite of 5-Fluorouracil (5-FUMP). The molecules with betterG-Scores were subjected to predict pharmacokinetic or ADME properties. The molecules with acceptable ADME properties and betterG-Scores were prioritized for synthesis and anticancer evaluation. Three molecules from pyrimidine carboxylate series PIC1-31were found acceptable withG-Scores and pharmacokinetic properties. Thus a library of pyrimidine derivatives was constructed based upon the feasibility of synthesis and in silico screened to prioritize the molecules and to obtain potential lead molecules as TS inhibitors.

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13

Popa, Marcel Mirel, Emilian Georgescu, Mino R. Caira, Florentina Georgescu, Constantin Draghici, Raluca Stan, Calin Deleanu i Florea Dumitrascu. "Indolizines and pyrrolo[1,2-c]pyrimidines decorated with a pyrimidine and a pyridine unit respectively". Beilstein Journal of Organic Chemistry 11 (26.06.2015): 1079–88. http://dx.doi.org/10.3762/bjoc.11.121.

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The three possible structural isomers of 4-(pyridyl)pyrimidine were employed for the synthesis of new pyrrolo[1,2-c]pyrimidines and new indolizines, by 1,3-dipolar cycloaddition reaction of their corresponding N-ylides generated in situ from their corresponding cycloimmonium bromides. In the case of 4-(3-pyridyl)pyrimidine and 4-(4-pyridyl)pyrimidine the quaternization reactions occur as expected at the pyridine nitrogen atom leading to pyridinium bromides and consequently to new indolizines via the corresponding pyridinium N-ylides. However, in the case of 4-(2-pyridyl)pyrimidine the steric hindrance directs the reaction to the pyrimidinium N-ylides and, subsequently, to the formation of the pyrrolo[1,2-c]pyrimidines. The new pyrrolo[1,2-c]pyrimidines and the new indolizines were structurally characterized through NMR spectroscopy. The X-ray structures of two of the starting materials, 4-(2-pyridyl)pyrimidine and 4-(4-pyridyl)pyrimidine, are also reported.

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Liu, Xianxian, i Rebecca E. Parales. "Chemotaxis of Escherichia coli to Pyrimidines: a New Role for the Signal Transducer Tap". Journal of Bacteriology 190, nr 3 (7.12.2007): 972–79. http://dx.doi.org/10.1128/jb.01590-07.

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ABSTRACT Escherichia coli exhibits chemotactic responses to sugars, amino acids, and dipeptides, and the responses are mediated by methyl-accepting chemotaxis proteins (MCPs). Using capillary assays, we demonstrated that Escherichia coli RP437 is attracted to the pyrimidines thymine and uracil and the response was constitutively expressed under all tested growth conditions. All MCP mutants lacking the MCP Tap protein showed no response to pyrimidines, suggesting that Tap, which is known to mediate dipeptide chemotaxis, is required for pyrimidine chemotaxis. In order to confirm the role of Tap in pyrimidine chemotaxis, we constructed chimeric chemoreceptors (Tapsr and Tsrap), in which the periplasmic and cytoplasmic domains of Tap and Tsr were switched. When Tapsr and Tsrap were individually expressed in an E. coli strain lacking all four native MCPs, Tapsr mediated chemotaxis toward pyrimidines and dipeptides, but Tsrap did not complement the chemotaxis defect. The addition of the C-terminal 19 amino acids from Tsr to the C terminus of Tsrap resulted in a functional chemoreceptor that mediated chemotaxis to serine but not pyrimidines or dipeptides. These results indicate that the periplasmic domain of Tap is responsible for detecting pyrimidines and the Tsr signaling domain confers on Tapsr the ability to mediate efficient chemotaxis. A mutant lacking dipeptide binding protein (DBP) was wild type for pyrimidine taxis, indicating that DBP, which is the primary chemoreceptor for dipeptides, is not responsible for detecting pyrimidines. It is not yet known whether Tap detects pyrimidines directly or via an additional chemoreceptor protein.

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Bischoff, Kerstin, Ulrich Girreser, Dieter Heber i Martin Schütt. "Two-Step Synthetic Approach to 6-Substituted Pyrido[2,3-d]pyrimidine(1H,3H)-2,4-diones from 6-Amino-, 6-Alkylamino-, and 6-Arylamino-1,3-dimethyluracils". Zeitschrift für Naturforschung B 61, nr 4 (1.04.2006): 486–94. http://dx.doi.org/10.1515/znb-2006-0415.

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The Mannich reaction of 7-aryl-5,6-dihydropyrido[2,3-d]pyrimidines 3, easily accessible by condensation of 6-amino-1,3-dimethyluracil (1) with Mannich bases 2a - c, gives rise to a mixture of 7-aryl-6-(N,N-dimethylaminomethyl)pyrido[2,3-d]pyrimidines 6 and 7 as well as 1,2-bis- (7-arylpyrido[2,3-d]pyrimidin-6-yl)ethane 13 the ratio of which depends on the reaction conditions and the amine used. 6-Alkylamino-1,3-dimethyluracils 15 - 18 were converted to the corresponding 5-(3-oxo-3-phenylpropyl)uracils 19 - 22 by condensation with the Mannich base 2a. Ring closure of 19 - 22 was performed by Vilsmeier formylation to afford the 8-alkyl- and 7,8-diaryl-5,8- dihydropyrido[2,3-d]pyrimidine-6-carbaldehydes 9 - 12 via the corresponding iminium salts 27 - 30

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Verbitskiy, Egor, Gennady Rusinov, Oleg Chupakhin i Valery Charushin. "Recent Advances in Direct C–H Functionalization of Pyrimidines". Synthesis 50, nr 02 (14.12.2017): 193–210. http://dx.doi.org/10.1055/s-0036-1589520.

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Data spanning the period 2000–2017 on the direct C–H functionalization of pyrimidines are collected and discussed in this review. This demonstrates the surge of interest and creativity that this field of chemistry has experienced during the last two decades. Plausible applications of highly functionalized pyrimidines are also discussed.1 Introduction2 Transition-Metal-Catalyzed C–H Functionalization of Pyrimidine Derivatives3 Transition-Metal-Free Direct C–H Functionalization of Pyrimidine Derivatives4 Deprotonative Metalation of Pyrimidine Derivatives5 Conclusions

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Dawood, Dina H., Eman M. H. Abbas, Thoraya A. Farghaly, Mamdouh M. Ali i Mohammed F. Ibrahim. "ZnO Nanoparticles Catalyst in the Synthesis of Bioactive Fused Pyrimidines as Anti-breast Cancer Agents Targeting VEGFR-2". Medicinal Chemistry 15, nr 3 (12.04.2019): 277–86. http://dx.doi.org/10.2174/1573406414666180912113226.

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Background: Pyrimidines emerged as a remarkable class of heterocyclic compounds that have reinforced the pharmaceutical chemistry with various bioactive antitumor agents. Moreover, pyrimidine scaffold displayed VEGFR-2 inhibitory activity. Also, nano-sized catalysts are used in organic reactions in order to speed up the catalytic process. Objective: We were interested herein to synthesize a new series of fused pyrimidines using ZnO(NPs) to investigate their antitumor efficiency against breast MCF7 cancer and their VEGFR- 2 inhibition properties. Method: A simple and efficient method for the synthesis of fused pyrimidines was developed using zinc oxide nanoparticles ZnO(NPs) in refluxing ethanol. Results: The proposed structures of all new fused pyrimidines are in agreement with their spectral data. Antitumor evaluation of newly fused pyrimidine derivatives against breast MCF-7 cancer was performed. It was apparent that the 2-phenylpyrazolo[1,5-a]pyrimidine derivatives 9a (IC50 = 9.12±1.16 µg/ml), 9c (IC50 = 9.10±1.07 µg/ml) and 9d (IC50 = 9.60±1.22 &µg/ml) exhibited equipotent antitumor activity as Tamoxifen (IC50 = 9.11±0.90 &µg/ml). Also, the inhibitory activity of the novel fused pyrimidine derivatives on VEGFR-2 as well as Tamoxifen was determined using breast cancer cell line MCF-7. The data was obvious that 2-phenylpyrazolo[1,5-a]pyrimidine derivatives 9a, 9c and 9d exhibited noticeable VEGFR-2 inhibitory effect with % inhibition ranging from 80-84 % versus Tamoxifen 93.5%. Conclusion: We succeeded in this context to synthesize new fused pyrimidines using ZnO(NPs) as anti-breast cancer agents targeting VEGFR-2.<p>

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Agarkov, Artem S., Dilyara O. Mingazhetdinova, Anna A. Nefedova, Alexander S. Ovsyannikov, Andrey K. Shiryaev, Igor A. Litvinov, Svetlana E. Solovieva i Igor S. Antipin. "Synthesis and Structure of 6-Acetyl-2-Arylhydrazone Derivatives of Thiazolo[3,2-a]Pyrimidine". Organics 4, nr 3 (11.08.2023): 438–46. http://dx.doi.org/10.3390/org4030031.

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Triazolo[4,3-a]pyrimidine is one of the promising structural fragments for the development of drugs, including anticancer drugs. This work is devoted to the synthesis of a number of new 2-arylhydrazone derivatives of thiazolo[3,2-a]pyrimidine, which are synthetic precursors for triazolo[4,3-a]pyrimidines. The crystal structure of 6-acetyl-7-methyl-5-phenyl-2-(2-phenylhydrazineylidene)-5H-thiazolo[3,2-a]pyrimidin-3(2H)-one was established by SCXRD. In the reduction reaction of the compound, the following system was used: vanadium(V) oxide, and sodium borohydride in ethanol at room temperature, which led to the formation of only one pair of diastereomers (1R*)-1-((5S*,6R*,7R*)-(1-(hydroxymethyl)-7-methyl-1,5-diphenyl-1,5,6,7-tetrahydro[1,2,4]triazolo[4,3-a]pyrimidin-6-yl)ethan-1-ol.

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Ogurtsov, Vladimir, i Oleg Rakitin. "4-Chloro-6-(chloromethyl)-1-methyl-1H-pyrazolo[3,4-d]pyrimidine". Molbank 2021, nr 3 (22.07.2021): M1253. http://dx.doi.org/10.3390/m1253.

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A novel 4-chloro-6-(chloromethyl)-1-methyl-1H-pyrazolo[3,4-d]pyrimidine was prepared by a rational and short two-step synthesis from commercially available ethyl 5-amino-1-methyl-1H-pyrazole-4-carboxylate via 6-(chloromethyl)-1-methyl-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one. The structure of the synthesized compounds was established by elemental analysis, high-resolution mass-spectrometry, 1H, 13C-NMR and IR spectroscopy and mass-spectrometry. 4-Chloro-6-(chloromethyl)-1-methyl-1H-pyrazolo[3,4-d]pyrimidine is a convenient intermediate for various disubstituted 1-methyl-1H-pyrazolo[3,4-d]pyrimidines, which may be of interest as substances with useful pharmacological properties.

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Povidaichyk, M., О. Onysko i M. Onysko. "SYNTHESIS OF TERMINAL 2-ALKENYL(ALKYNYL)THIO-5-CYANO-6-(p-DIMETHYLAMINOPHENYL)PYRIMIDIN-4-ONES". Scientific Bulletin of the Uzhhorod University. Series «Chemistry» 48, nr 2 (23.05.2023): 79–83. http://dx.doi.org/10.24144/2414-0260.2022.2.79-83.

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Functionalized pyrimidines possess a wide spectrum of biological activity. In particular, they have antitumor, antiviral, and anticonvulsant activities, exhibit anti-inflammatory and analgesic effects, and they are inhibitors of aldose reductase, SecA ATPase, azide, and plant growth. The search for methods of synthesis of new functionalized and condensed pyrimidine derivatives is an urgent problem. Alkenyl-functionalized mono- and polycyclic pyrimidines are promise substrates for studying the regioselectivity of electroph ilic heterocyclization reactions under the influence of halogen-containing electrophilic agents, and halogen- and chalcogen-functionalized cyclization products showed high antibacterial, antifungal, and antimalarial activity. The introduction of new functional groups capable to modification into such alkenylpyrimidines can significantly affect their reactivity and change/enhance the biological activity of the halocyclization products. We proposed the synthesis of 2-alkenyl(alkynyl)thio derivatives of 5-cyano-6-(p-dimethylaminophenyl)-pyrimidin-4-one containing a cyano group labile to functionalization. As a result of alkylation of 2-thioxo-5-cyano-6-(p-dimethylaminophenyl)pyrimidin-4-one with unsaturated alkyl halides in an alkaline medium, the terminal alkenyl (allyl, methallyl) and alkynyl (propargyl) thioethers of cyanopyrimidine were obtained, promising for heterocyclization with halogen-containing electrophilic reagents . Keywords: 2-thioxo-5-cyano-pyrimidin-4-one; alkylation; alkenylthiopyrimidinone; alkynylthiopyrimidinone.

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Mosaad Sayed Mohamed, Samir Mohamed Awad, Neama Abdallah Abd El-tawab i Naglaa Mohamed Ahmed. "An overview on synthesis and biological activity of pyrimidines". World Journal of Advanced Research and Reviews 15, nr 1 (30.07.2022): 272–96. http://dx.doi.org/10.30574/wjarr.2022.15.1.0689.

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Pyrimidines represent an important class of heterocycles containing two nitrogen atoms at position 1 and 3 of the six membered ring show wide range of biological activities. Numerous methods for the synthesis of pyrimidine and their diverse reactions offer enormous scope in the field of medicinal chemistry. Pyrimidine possesses wide spectrum of biological activities including antitubercular, antibacterial, antifungal, antiviral, anti-inflammatory, antimalarial, anticancer, and anti-HIV activity. The present review attempts to give brief information about the synthesis and various biological activities of pyrimidines and their derivatives.

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Mohamed, Mosaad, Ramdan El-Domany i Rania Abd El-Hameed. "Synthesis of certain pyrrole derivatives as antimicro-bial agents". Acta Pharmaceutica 59, nr 2 (1.06.2009): 145–58. http://dx.doi.org/10.2478/v10007-009-0016-9.

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Synthesis of certain pyrrole derivatives as antimicro-bial agentsIn an effort to establish new pyrroles and pyrrolo[2,3-d] pyrimidines with improved antimicrobial activity we report here the synthesis andin vitromicrobiological evaluation of a series of pyrrole derivatives. A series of new 2-aminopyrrole-3-carbonitriles (1a-d) were synthesized from the reaction of benzoin, primary aromatic amines and malononitrile, from which a number of pyrrole derivatives (2a-dto5a-d) and pyrrolo[2,3-d]pyrimidines (6a-dto10a, d) were synthesized. Thein vitroantimicrobial testing of the synthesized compounds was carried out against Gram-positive, Gram-negative bacteria and fungi. Some of the prepared compounds, [2-amino-1-(2-methylphenyl)-4,5-diphenyl-1H-pyrrole-3-carbonitriles (1b), 2-amino-3-carbamoyl-1-(3-methylphenyl)-4,5-diphenyl-1H-pyrroles (2b),N-(3-cyano-1-(2-methylphenyl)-4,5-diphenyl-1H-pyrrol-2-yl)-acetamides (3b),N-(3-cyano-1-(3-methylphenyl)-4,5-diphenyl-1H-pyrrol-2-yl)-acetamides (3c), 2-amino-1-(4-methoxyphenyl)-4,5-diphenyl-3-tetrazolo-1H-pyrroles (5d),7-(4-methoxyphenyl)-5,6-diphenyl-7H-pyrrolo [2,3-d]pyrimidin-4(3H)-ones (7d), 7-(3-methylphenyl)-5,6-diphenyl-7H-pyrrolo[2,3-d]pyrimidin-4(3H)-thione (9b) andN-(7-(2-methylphenyl)-5,6-diphenyl-7H-pyrrolo[2,3-d] pyrimidine)-N-aryl amines (10a)] showed potent antimicrobial activity.

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A-Ani, Zaid S. M., Sana A. Abdulmawjood, Adel O. A. Al-Hussain i Shihab A. Al-Bajari. "Synthesis and Biological Activity of few Pyrimidines Derivatives against Hepatic Injury Stimulated by Carbon Tetrachloride in Male Rats". INTERNATIONAL JOURNAL OF DRUG DELIVERY TECHNOLOGY 12, nr 04 (25.12.2022): 1496–501. http://dx.doi.org/10.25258/ijddt.12.4.02.

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In the presence of sodium hydroxide, substituted chalcones are reacted with cyanoguandine in ethanol, and some chalcone compounds are used as a nucleus in the preparation of some five-, hexa-, and hepta-, heterocyclic compounds pyrimidine (pyrimidines derivatives), pyrimidine derivatives (A1, A2, and A3). Contains therapeutic properties and bioactivity, and has been used to treat various ailments. This study aimed to learn more about how pyrimidine derivatives could help mitigate the undesirable implications of carbon tetrachloride. a group of 50 male rats were separated into 5 groups: healthy control (no treated), CCl4 group, and the rest. A1 (N-(6-(5-methylthiophen-2yl)-4-phenyl-3,4-dihydropyrimidin- (1H)-ylidene) cyanamide), A2 (N-(6-(5-methylthiophen-2yl)-4-(4-nitrophenyl)-3,4-dihydropyrimidin -2(1H)-ylidene)cyanamide), A3 (N-(4-( Melting points, (FTIR) spectroscopy, 1HNMR spectroscopy, and thin layer chromatography method (TLC) were used to describe compounds [A1, A2 and A3] to monitor the impacted liver function. Pyrimidines derivatives compounds reduced CCl4 toxicity while increasing the levels of aspartate transaminase, alanine transaminase, gamma-glutamyltransferase, and alkaline phosphatase, unlike the CCl4 group and the CCl4 groups containing pyrimidines derivatives. The quantities of total lipids, protein, globulin, and albumin in the control group were substantially different (P0.05). Lipid peroxidation produced a considerable quantity of malondialdehyde compared to the control group, the CCl4 group. However, pyrimidines derivatives components reduced the quantity CCl4, lowering oxidative stress. The levels of catalase, glutathione, and glutathione peroxidase were higher in individuals who were given just CCl4 elevated in groups of pyrimidines derivatives component. There were substantial disparities in superoxide dismutase levels throughout the groups studied.

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Hocková, Dana, Milena Masojídková i Antonín Holý. "Sonogashira Cross-Coupling in the Synthesis of Acyclic Nucleoside Phosphonates: Preparation of 6-[(Phosphonomethoxy)alkynyl]- and 6-[(Phosphonomethoxy)alkyl]pyrimidines". Collection of Czechoslovak Chemical Communications 70, nr 2 (2005): 247–58. http://dx.doi.org/10.1135/cccc20050247.

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Several 6-[(phosphonomethoxy)alkyl]pyrimidines and 6-[(phosphonomethoxy)alkynyl]pyrimidines were prepared as saturated and unsaturated carba-analogues of antivirally active 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]pyrimidine. As the key step of their synthesis the Sonogashira cross-coupling reaction was successfully applied. The replacement of the C-O moiety by the C-C bond resulted in the loss of biological activity.

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Chandrani, Jeenkal P., i Kalpesh J. Ganatra. "An Efficient And Catalytically Free Chemical Transformation of Pyrimidin-2(1H)-one to 2-(N-Arylamino)pyrimidines and their in vitro Cytotoxicity Evaluation". Asian Journal of Organic & Medicinal Chemistry 5, nr 2 (2020): 133–37. http://dx.doi.org/10.14233/ajomc.2020.ajomc-p260.

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With the aim to develop an efficient strategy to synthesize pyrimidine derivatives bearing diversely substituted amines involves four step linear protocols started with Biginelli multi-component reaction leading to dihydropyrimidines which passing throug multistep sequantial process containing oxidation, chlorination and catalytically free transformation of pyrimidin-2(1H)-one to 2-(N-arylamino)pyrimidines, were evaluated for cytotoxicity study against human cancer lines HCT-116, Hep-G2 and QG-56. Compound 4j exhibit significant anticancer activity showed against: human hepato carcinoma (Hep-G2) and human colon carcinoma (HCT-116) serve as a excellent lead molecule for the generation of various promising targets.

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26

Latif, Muhammad, Byung Jin Byun i Kwangho Lee. "Synthesis of 4‐(3,4‐dicarboxamido‐1H‐pyrrole)pyrimidines as Anaplastic Lymphoma Kinase Inhibitors". Bulletin of the Korean Chemical Society 36, nr 2 (29.01.2015): 520–25. http://dx.doi.org/10.1002/bkcs.10097.

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To explore non‐aniline aromatic substitution on the pyrimidine C4 position, novel 4‐(N,N′‐di‐n‐propyl‐3,4‐dicarboxamido‐1H‐pyrrole)pyrimidines are designed and synthesized as anaplastic lymphoma kinase inhibitors for non‐small cell lung cancer treatment. To overcome the unexpected cleavage between the C‐N linkage of pyrrole nitrogen and C4‐pyrimidine during hydrolysis and inaccessibility of the desired diamide formation through coupling agent‐mediated conditions, the 4‐(N,N′‐di‐n‐propyl‐3,4‐dicarboxamido‐1H‐pyrrole)pyrimidine was assembled through direct nucleophilic substitution under microwave irradiation. Thus prepared 4‐(N,N′‐di‐n‐propyl‐3,4‐dicarboxamido‐1H‐pyrrole)pyrimidines were measured both ALK binding and H3122 cell proliferation assay. Their weak ALK activities are explained with molecular modeling study.

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Hussein, Khlood Abdulla Ahmed, i Yacoob Abdulla Kassium. "Synthesis and characterization of some New 2- and 6- substituted of 5- Acetyl - 4- (P- phenyl) Pyrimidine and substituted thieno [2, 3- d] Pyrimidine". University of Aden Journal of Natural and Applied Sciences 25, nr 2 (31.10.2021): 273–82. http://dx.doi.org/10.47372/uajnas.2021.n2.a05.

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The series of new pyrimidines derivatives 2- and 6- Substituted of 5 - Acetyl - 4 - (P- phenyl) Pyrimidine and Substituted thieno [2, 3- d] Pyrimidine are synthesis by the reaction between some substituted of benzaldehydes with ethyl aceto acetate in the present of ethanol as a solvent to give the products(3e-h), when react alkyl halide with (3e-h) in ethanol obtain new Pyrimidine derivatives(4e-h) heating them with phosphorous oxy chloride in dioxane to form (5e-h) which reacts with thiourea in ethanol to produce (6e-h) these compounds reacting with chloro acetic acid to form new Substituted thieno [2,3-d] Pyrimidine (8e-h). All the synthesized compounds of new pyrimidines derivatives are identified by the physical properties by it's melting points, colors and the yields are characterized by the elemental (CHN)analysis, IR, UV Spectrum.

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Hussein, Khlood Abdulla Ahmed, i Yacoob Abdulla Kassium. "Synthesis and characterization of some New 2- and 6- substituted of 5- Acetyl - 4- (P- phenyl) Pyrimidine and substituted thieno [2, 3- d] Pyrimidine". University of Aden Journal of Natural and Applied Sciences 25, nr 2 (31.10.2021): 273–82. http://dx.doi.org/10.47372/uajnas.2021.n2.a05.

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The series of new pyrimidines derivatives 2- and 6- Substituted of 5 - Acetyl - 4 - (P- phenyl) Pyrimidine and Substituted thieno [2, 3- d] Pyrimidine are synthesis by the reaction between some substituted of benzaldehydes with ethyl aceto acetate in the present of ethanol as a solvent to give the products(3e-h), when react alkyl halide with (3e-h) in ethanol obtain new Pyrimidine derivatives(4e-h) heating them with phosphorous oxy chloride in dioxane to form (5e-h) which reacts with thiourea in ethanol to produce (6e-h) these compounds reacting with chloro acetic acid to form new Substituted thieno [2,3-d] Pyrimidine (8e-h). All the synthesized compounds of new pyrimidines derivatives are identified by the physical properties by it's melting points, colors and the yields are characterized by the elemental (CHN)analysis, IR, UV Spectrum.

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Cawrse, Brian M., Nia’mani M. Robinson, Nina C. Lee, Gerald M. Wilson i Katherine L. Seley-Radtke. "Structural and Biological Investigations for a Series of N-5 Substituted Pyrrolo[3,2-d]pyrimidines as Potential Anti-Cancer Therapeutics". Molecules 24, nr 14 (23.07.2019): 2656. http://dx.doi.org/10.3390/molecules24142656.

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Pyrrolo[3,2-d]pyrimidines have been studied for many years as potential lead compounds for the development of antiproliferative agents. Much of the focus has been on modifications to the pyrimidine ring, with enzymatic recognition often modulated by C2 and C4 substituents. In contrast, this work focuses on the N5 of the pyrrole ring by means of a series of novel N5-substituted pyrrolo[3,2-d]pyrimidines. The compounds were screened against the NCI-60 Human Tumor Cell Line panel, and the results were analyzed using the COMPARE algorithm to elucidate potential mechanisms of action. COMPARE analysis returned strong correlation to known DNA alkylators and groove binders, corroborating the hypothesis that these pyrrolo[3,2-d]pyrimidines act as DNA or RNA alkylators. In addition, N5 substitution reduced the EC50 against CCRF-CEM leukemia cells by up to 7-fold, indicating that this position is of interest in the development of antiproliferative lead compounds based on the pyrrolo[3,2-d]pyrimidine scaffold.

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Zakharov, Timofei N., Pavel A. Sakharov, Mikhail S. Novikov, Alexander F. Khlebnikov i Nikolai V. Rostovskii. "Triethylamine-Promoted Oxidative Cyclodimerization of 2H-Azirine-2-carboxylates to Pyrimidine-4,6-dicarboxylates: Experimental and DFT Study". Molecules 28, nr 11 (24.05.2023): 4315. http://dx.doi.org/10.3390/molecules28114315.

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An unprecedented oxidative cyclodimerization reaction of 2H-azirine-2-carboxylates to pyrimidine-4,6-dicarboxylates under heating with triethylamine in air is described. In this reaction, one azirine molecule undergoes formal cleavage across the C-C bond and another across the C=N bond. According to the experimental study and DFT calculations, the key steps of the reaction mechanism include nucleophilic addition of N,N-diethylhydroxylamine to an azirine to form an (aminooxy)aziridine, generation of an azomethine ylide, and its 1,3-dipolar cycloaddition to the second azirine molecule. The crucial condition for the synthesis of pyrimidines is generation of N,N-diethylhydroxylamine in the reaction mixture in a very low concentration, which is ensured by the slow oxidation of triethylamine with air oxygen. Addition of a radical initiator accelerated the reaction and resulted in higher yields of the pyrimidines. Under these conditions, the scope of the pyrimidine formation was elucidated, and a series of pyrimidines was synthesized.

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Greco, Chiara, Rosa Catania, Dario Leonardo Balacco, Vincenzo Taresco, Francesca Musumeci, Cameron Alexander, Alan Huett i Silvia Schenone. "Synthesis and Antibacterial Evaluation of New Pyrazolo[3,4-d]pyrimidines Kinase Inhibitors". Molecules 25, nr 22 (16.11.2020): 5354. http://dx.doi.org/10.3390/molecules25225354.

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Pyrazolo[3,4-d]pyrimidines represent an important class of heterocyclic compounds well-known for their anticancer activity exerted by the inhibition of eukaryotic protein kinases. Recently, pyrazolo[3,4-d]pyrimidines have become increasingly attractive for their potential antimicrobial properties. Here, we explored the activity of a library of in-house pyrazolo[3,4-d]pyrimidines, targeting human protein kinases, against Staphylococcus aureus and Escherichia coli and their interaction with ampicillin and kanamycin, representing important classes of clinically used antibiotics. Our results represent a first step towards the potential application of dual active pyrazolo[3,4-d]pyrimidine kinase inhibitors in the prevention and treatment of bacterial infections in cancer patients.

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Tomlinson, Patricia Tolson, i Carol J. Lovatt. "Nucleotide Metabolism in ‘Washington’ Navel Orange Fruit: I. Pathways of Synthesis and Catabolism". Journal of the American Society for Horticultural Science 112, nr 3 (maj 1987): 529–35. http://dx.doi.org/10.21273/jashs.112.3.529.

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Abstract The capacity of ‘Washington’ navel orange fruit [Citrus sinensis (L.) Osbeck] to synthesize and catabolize purines and pyrimidines was assessed. De novo biosynthesis of purine nucleotide was demonstrated by [14C] bicarbonate incorporation into purine nucleotides, blockage of this process by four known inhibitors, and assimilation of radiolabeled carbon from formate, both carbons of glycine, and carbon-3 of serine into the adenine ring. De novo synthesis of pyrimidines via the orotate pathway in young fruit was demonstrated by incorporation of [14C] bicarbonate and [6-14C]orotic acid into uridine nucleotides, release of 14CO2 from [7-14C]orotic acid, and blockage of these processes by 6-azauridine. Synthesis of purine and pyrimidine nucleotides via salvage reactions was demonstrated by incorporation of radiolabeled bases and ribonucleosides into nucleotides and into nucleic acids. Release of 14CO2 from radiolabeled adenine, adenosine, hypoxanthine, and xanthine, uric acid, urea (purines), uracil, and uridine (pyrimidines) provided evidence the pathways for catabolism (degradation) of purines and pyrimidines in navel orange fruit are similar to those found in microorganisms and animal tissues. To the best of our knowledge, this report is the first to assess the capacity of anabolic and catabolic pathways of purine and pyrimidine nucleotide metabolism in fruit of any species. De novo synthetic activities in orange fruit permit increases in the pools of purine and pyrimidine nucleotides using simple precursors. Further, the patterns of salvage and catabolism suggest riboside pools are reused predominantly as nucleotides, while the majority of base pools are degraded to permit recycling of carbon and nitrogen into other metabolites.

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Tiwari, Sangeeta, Ashok K. Yadav i A. K. Mishra. "Some New Pyrido[2,3-d]pyridimines and their Nucleoside of Biological Importance". E-Journal of Chemistry 7, s1 (2010): S85—S92. http://dx.doi.org/10.1155/2010/812567.

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Chalcones (I) reacted with malanonitrile and ammonium acetate yielded 2-amino-3-cyano-4,6-disubstituted pyridines (II) in excellent yield. 4-Amino-5,7-disubstituted pyrido [2,3-d]pyrimidine-2(1H)-thiones (III), 4-amino-5,7-disubstituted pyrido[2,3-d]pyrimidines (IV) and 4-imino-3,5,7-trisubstituted pyrido[2,3-d]pyrimidin-2(1H)-ones (V) have been synthesized by the condensation of compound (II) with thiourea, formamide and arylisocynate respectively. The ribofuranosidesviz. 4-amino-5,7-disubstituted-1- [2',3',5'-tri-o-benzoyl-β,D-ribofuranosyl]pyrido[2,3-d]pyrimidine-2-(1H)-thiones (VI) and 4-imino-3,5,7- trisubstituted-1- [2',3',5'-tri-o-benzoyl-β,D-ribofuranosyl] pyrido [2,3-d] pyrimidine-2(1H)-one (VII) were synthesized by converting compounds III and V to trimethylsilyl derivative in situ by reacting them with hexamethyldisilazane to give corresponding ribofuranosides withβ-D-ribofuranose-1-acetate-2,3,5-tribenzoate. Compounds III-V and their ribofuranosides have been screened for antimicrobial and antifungal evaluations.

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Chaudhary, Ankita. "Multicomponent Approach for the Sustainable Syntheses of Pyrido[2,3-d]pyrimidine Scaffold". Current Organic Chemistry 25, nr 23 (16.12.2021): 2856–84. http://dx.doi.org/10.2174/1385272825666211117152900.

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Pyrido[2,3-d]pyrimidine is an N-fused heterocyclic compound formed by the ortho fusion of pyridine and pyrimidine ring. Pyrido[2,3-d]pyrimidines hold a prominent position in medicinal chemistry owing to their wide spectrum of biological activities like antiviral, antihistaminic, antibacterial, diuretic, anti-inflammatory, analgesic, anticonvulsive, antipyretic, etc. The extraordinary features of pyrido[2,3-d]pyrimidines make their synthesis a perpetual field of research. Moreover, the construction of elaborate biologically relevant moieties via a multicomponent approach has become a promising area of research, owing to the burgeoning ‘green chemistry drive’. Advances in the exploitation of proficient synthetic routes involving a multicomponent approach for the assembly of this scaffold are reported in this review.

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Soto-Acosta, Ruben, Eunkyung Jung, Li Qiu, Daniel J. Wilson, Robert J. Geraghty i Liqiang Chen. "4,7-Disubstituted 7H-Pyrrolo[2,3-d]pyrimidines and Their Analogs as Antiviral Agents against Zika Virus". Molecules 26, nr 13 (22.06.2021): 3779. http://dx.doi.org/10.3390/molecules26133779.

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Discovery of compound 1 as a Zika virus (ZIKV) inhibitor has prompted us to investigate its 7H-pyrrolo[2,3-d]pyrimidine scaffold, revealing structural features that elicit antiviral activity. Furthermore, we have demonstrated that 9H-purine or 1H-pyrazolo[3,4-d]pyrimidine can serve as an alternative core structure. Overall, we have identified 4,7-disubstituted 7H-pyrrolo[2,3-d]pyrimidines and their analogs including compounds 1, 8 and 11 as promising antiviral agents against flaviviruses ZIKV and dengue virus (DENV). While the molecular target of these compounds is yet to be elucidated, 4,7-disubstituted 7H-pyrrolo[2,3-d]pyrimidines and their analogs are new chemotypes in the design of small molecules against flaviviruses, an important group of human pathogens.

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Lee, Su-Jeong, Jun-Gi Ahn, Jihwan Seo, Heun-Jong Ha i Chang-Woo Cho. "Organocatalytic enantioselective synthesis of acyclic pyrimidine nucleosides by aza-Michael reaction". Organic & Biomolecular Chemistry 16, nr 48 (2018): 9477–86. http://dx.doi.org/10.1039/c8ob02754d.

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Geies, Ahmed A. "Bromonitriles in Heterocyclic Synthesis. Synthesis and Reactions of Thiazolo[3,2-a]pyrimidines (III)". Collection of Czechoslovak Chemical Communications 57, nr 7 (1992): 1565–69. http://dx.doi.org/10.1135/cccc19921565.

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As a continuation of our previous work about the synthesis and properties of thiazolopyrimidines, which are expected to be of biological and medicinal importance, the present work is aimed to synthesize new polyfunctional substituted thiazolo[3,2-a]pyrimidines. Pyrimidine derivatives I were reacted with bromomalononitrile or ethyl bromocyanoacetate at room temperature in ethanol in presence of potassium hydroxide as a basic catalyst followed by refluxing the reaction mixture to give thiazolo[3,2-a]pyrimidines IIa-IId.

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Yavolovskii, Arkadii, Araksia Davtian, Lidiya Grishchuk, Sergei Pluzhnik-Glagyr, Ildar Rakipov, Yuri Ivanov, Dmytro Chikhichin i Gerbert Kamalov. "AMINATION OF 2-(2-OXO-2-ARYLETHYLTHIO)-PYRIMIDIN-4(3H)-ONE DERIVATIVES USING THE SULFONATE METHOD". Ukrainian Chemistry Journal 89, nr 1 (24.02.2023): 60–67. http://dx.doi.org/10.33609/2708-129x.89.01.2023.60-67.

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A Derivatives of 2-thiouracil are characterized by wide spectrum of biological activity, which is characteristic of most representatives this heterocycles class. In particular, 2-(2-oxo-2-phenylethylthio)-pyrimidin-4(3H)-ones belong to the group of non-nucleoside inhibitors of HIV-1 reverse transcriptase. The antimalarial properties of 2-(2-oxo-2-phenylethylthio)-4-R-pyrimidine derivatives, which proved to be effective inhibitors of CIpP protease of Plasmodium falciparum, are being studied. Known examples of 2-(2-oxo-2-phenylethylthio)-pyrimidines modification at the "4" position of the heterocycle are limited to use 4-chloro derivatives, which, in turn, are formed according to the classical method by reaction of pyrimidine-4(3H)-ones with POCl3 at boiling point of reaction mixture. In this work, we present an alternative version of modification the above-mentioned class of compounds. By amination amide function of 6-R-2-(2-oxo-2-arylethylthio)-pyrimidin-4(3H)-ones derivatives of with ethanolamine and 1-aminopropane-2,3-diol using sulfonate method, synthesized and characterized new compounds a 6-R-2-(2-oxo-2-phenylethylthio)-pyrimidines series by spectral methods. The advantages of this scheme are discussed (the formation of intermediate sulfonates and the amination stage do not require harsh conditions and are carried out with satisfactory yields). The proposed scheme can be recommended in cases where the original substrate contains functional groups that are labile at high temperatures and sensitive to an acidic environment.

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Velihina, Y. S., S. G. Pilyo, I. V. Ivanova i V. S. Brovarets. "Synthesis of pyrazolo[1,5-a][1,3,5]triazine and oxazolo[4,5-d]pyrimidine derivatives and study of their vasodilator activity". Voprosy Khimii i Khimicheskoi Tekhnologii, nr 2 (maj 2023): 51–60. http://dx.doi.org/10.32434/0321-4095-2023-147-2-51-60.

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A number of pyrazolo[1,5-a][1,3,5]triazine and oxazolo[4,5-d]pyrimidine derivatives were synthesized and characterized. Pyrazolo[1,5-a][1,3,5]triazines with various substituents in the fourth position and a dichloromethyl group in the second position were obtained by the heterocyclization reaction of available N-(2,2-dichloro-1-cyanoethenyl)carboxamides and 5-aminopyrazoles. Oxazolo[4,5-d]pyrimidines were obtained by treating 2-phenyl-4-dichloromethylene-1,3-oxazol-5(4H)-one with the corresponding arylamidine hydrochloride in the presence of triethylamine. The resulting 4,5-dihydro-1H-imidazol-5(4)-ones undergo recyclization with subsequent cyclocondensation to the corresponding oxazolo[4,5-d]pyrimidin-7-ones when heated in pyridine. Oxazolo[4,5-d]pyrimidines with a labile chlorine atom in position 7, whose substitution with various amines leads to 7-aminoderivatives of oxazolo[4,5-d]pyrimidine, were obtained by heating the latter in phosphorus (V) oxychloride in the presence of N,N-dimethylaniline. The study of the effect of the synthesized compounds on vascular tone showed that some of the studied samples exhibited vasodilator activity of varying strength. It was established that 2-dichloromethyl-7-methyl-4-(furan-2-yl)pyrazolo[1,5-a][1,3,5]triazine and 2-dichloromethyl-7-methyl-4-(pyridin-3-yl)pyrazolo[1,5-a][1,3,5]triazine showed a pronounced dose-dependent vasodilator effect and therefore, subject to their further research, may be promising for the development of new vasodilator drugs. The study of the biological activity of oxazolo[4,5-d]pyrimidine derivatives did not reveal potential vasodilator agents among the presented compounds, as they demonstrated a low vasodilator effect or did not show vasoactivity.

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Lagardère, Prisca, Cyril Fersing, Nicolas Masurier i Vincent Lisowski. "Thienopyrimidine: A Promising Scaffold to Access Anti-Infective Agents". Pharmaceuticals 15, nr 1 (27.12.2021): 35. http://dx.doi.org/10.3390/ph15010035.

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Thienopyrimidines are widely represented in the literature, mainly due to their structural relationship with purine base such as adenine and guanine. This current review presents three isomers—thieno[2,3-d]pyrimidines, thieno[3,2-d]pyrimidines and thieno[3,4-d]pyrimidines—and their anti-infective properties. Broad-spectrum thienopyrimidines with biological properties such as antibacterial, antifungal, antiparasitic and antiviral inspired us to analyze and compile their structure–activity relationship (SAR) and classify their synthetic pathways. This review explains the main access route to synthesize thienopyrimidines from thiophene derivatives or from pyrimidine analogs. In addition, SAR study and promising anti-infective activity of these scaffolds are summarized in figures and explanatory diagrams. Ligand–receptor interactions were modeled when the biological target was identified and the crystal structure was solved.

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Innocenti, Paolo, Hannah Woodward, Lisa O'Fee i Swen Hoelder. "Expanding the scope of fused pyrimidines as kinase inhibitor scaffolds: synthesis and modification of pyrido[3,4-d]pyrimidines". Organic & Biomolecular Chemistry 13, nr 3 (2015): 893–904. http://dx.doi.org/10.1039/c4ob02238f.

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A versatile and efficient entry into 2-amino-pyrido[3,4-d]pyrimidines was developed. Our strategy hinges on the concise preparation and derivatisation of 8-chloro-2-(methylthio)pyrido[3,4-d]pyrimidine intermediates to yield putative kinase inhibitors.

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42

Sahu, Pramod K., Praveen K. Sahu, Manvendra S. Kaurav, Mouslim Messali, Saud M. Almutairi, Puran L. Sahu i Dau D. Agarwal. "One-pot facile and mild construction of densely functionalized pyrimidines in water via consecutive C–C and C–S bonds formation". RSC Advances 8, nr 59 (2018): 33952–59. http://dx.doi.org/10.1039/c8ra04363a.

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Fused pyrimidines composed of alternating heteroatoms and a pyrimidine moiety were synthesized efficiently using readily available starting material 4-hydroxycoumarin, aromatic aldehydes, and urea/thiourea at room temperature.

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43

Pandhurnekar, Chandrashekhar P., Ekta M. Meshram, Himani N. Chopde i Rameshkumar J. Batra. "Synthesis, Characterization, and Biological Activity of 4-(2-Hydroxy-5-(aryl-diazenyl)phenyl)-6-(aryl)pyrimidin-2-ols Derivatives". Organic Chemistry International 2013 (1.07.2013): 1–10. http://dx.doi.org/10.1155/2013/582079.

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With the aim of synthesizing new heterocyclic compounds and exploring biological potency, new series of chalcones, that is, 3-(2-hydroxy-5-(aryl-diazenyl)phenyl)-1-(aryl)prop-2-en-1-one and their pyrimidine derivatives, that is, 4-(2-hydroxy-5-(aryl-diazenyl)phenyl)-6-(aryl)pyrimidin-2-ols were synthesized using different aromatic amines and salicylaldehyde as starting moieties. The structures of newly synthesized compounds were confirmed using different spectroscopic techniques such as IR, 1H-NMR, 13C-NMR, and mass spectral analysis, and elemental analysis. The newly synthesized pyrimidines derivatives were screened for their in vitro antibacterial and antifungal activities. It was observed that some of the newly synthesized compounds had shown promising activity against several bacterial and fungal stains. Anti-bacterial activity and anti-fungal activity studies revealed that pyrimidine derivatives consisting of nitro group in their molecular structure possess better activity than their corresponding chalcones.

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44

Schmidt, Andreas, i Thorsten Mordhorst. "Syntheses and Properties of Di- and Tricationic Hetarenium-Substituted Pyrimidines". Zeitschrift für Naturforschung B 61, nr 4 (1.04.2006): 396–405. http://dx.doi.org/10.1515/znb-2006-0405.

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2,4-Dichloro-, 4,6-dichloro-, 2,4,6-trichloro- and tetrachloropyrimidine undergo nucleophilic displacements by 4-(dimethylamino)pyridine to give (pyrimidine-2,4-diyl)-1,1’-bis[4-(dimethylamino) pyridinium] dichloride, (pyrimidine-4,6-diyl)-1,1’-bis[4-(dimethylamino)-pyridinium] dichloride, (pyrimidine-2,4,6-triyl)-1,1’,1”-tris[4-(dimethylamino)pyridinium] trichloride, and (5- chloropyrimidine-2,4,6-triyl)-1,1’,1”-tris[4-(dimethylamino)pyridinium] trichloride, respectively. Nucleophilic substitutions of the pyridinium substituents by O- and S-nucleophiles to functionalized pyrimidines are examined

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45

Romero-Ortega, Moisés, Michelle Trujillo-Lagunas, Ignacio Medina-Mercado, Ivann Zaragoza-Galicia i Horacio Olivo. "A Synthesis of 4-Chloro-2-(trichloromethyl)pyrimidines and Their Study in Nucleophilic Substitution". Synthesis 51, nr 02 (11.09.2018): 530–37. http://dx.doi.org/10.1055/s-0037-1610270.

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A convenient two-step, one-pot synthesis of 4-chloro-2-(trichloromethyl)pyrimidines starting from 2-(trichloromethyl)-1,3-diazabutadienes is described. These nitrogen heterocycles were prepared by a sequential acylation/intramolecular cyclization reaction between 2-(trichloromethyl)-1,3-diazabutadienes and acyl chlorides in the presence of triethylamine followed by treatment with POCl3. This is the first report for the synthesis of this type of 4-chloro-2-(trichloromethyl)pyrimidine derivatives and serves as a source for a wide variety of other substituted pyrimidines by nucleophilic substitution reactions.

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46

K, Ishwar Bhat, i Abhishek Kumar. "PYRIMIDINES AS POTENT CYTOTOXIC AND ANTI-INFLAMMATORY AGENTS". Asian Journal of Pharmaceutical and Clinical Research 10, nr 6 (1.06.2017): 237. http://dx.doi.org/10.22159/ajpcr.2017.v10i6.17343.

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Objective: Many derivatives of pyrimidine are known for the broad-spectrum biological activities such as antimicrobial, antitumor, antibacterial, antitubercular, anti-inflammatory, and cytotoxic activity. Chalcones with an enone group show potent pharmacological activities such as antiinflammatory, antibacterial, antifungal, and antimalarial activity. A series of pyrimidines from chalcones have been synthesized and screened for anti-inflammatory and cytotoxic activity studies.Methods: Chalcones [1-(4-nitrophenyl)-3-substituted-phenylprop-2-en-1-one] were synthesized from various substituted aldehydes with 4-nitroacetophenone and cyclized with urea and glacial acetic acid to give pyrimidine derivatives [4-(4-nitrophenyl)-6-substituted-phenylpyrimidin-2-ol].Results: Anti-inflammatory and cytotoxic activity studies revealed that some of the synthesized compounds have shown significant activity.Conclusion: The observed results proved that pyrimidines are found to be interesting lead molecules for the synthesis of anti-inflammatory and cytotoxic agents

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47

Nammalwar, Baskar, i Richard A. Bunce. "Recent Advances in Pyrimidine-Based Drugs". Pharmaceuticals 17, nr 1 (11.01.2024): 104. http://dx.doi.org/10.3390/ph17010104.

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Pyrimidines have become an increasingly important core structure in many drug molecules over the past 60 years. This article surveys recent areas in which pyrimidines have had a major impact in drug discovery therapeutics, including anti-infectives, anticancer, immunology, immuno-oncology, neurological disorders, chronic pain, and diabetes mellitus. The article presents the synthesis of the medicinal agents and highlights the role of the biological target with respect to the disease model. Additionally, the biological potency, ADME properties and pharmacokinetics/pharmacodynamics (if available) are discussed. This survey attempts to demonstrate the versatility of pyrimidine-based drugs, not only for their potency and affinity but also for the improved medicinal chemistry properties of pyrimidine as a bioisostere for phenyl and other aromatic π systems. It is hoped that this article will provide insight to researchers considering the pyrimidine scaffold as a chemotype in future drug candidates in order to counteract medical conditions previously deemed untreatable.

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Dodonova, Jelena, i Sigitas Tumkevicius. "Fused Pyrrolo[2,3-d]pyrimidines (7-Deazapurines) by Palladium-Catalyzed Direct N–H and C–H Arylation Reactions". Synthesis 49, nr 11 (2.03.2017): 2523–34. http://dx.doi.org/10.1055/s-0036-1588734.

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Palladium-catalyzed intramolecular direct C–H arylations for the synthesis of hitherto unknown fused hetero systems containing an incorporated pyrrolo[2,3-d]pyrimidine scaffold are described. Pyrimido[5′,4′:4,5]pyrrolo[2,1-a]isoindoles were synthesized from 2,4-diarylpyrrolo[2,3-d]pyrimidines and o-bromobenzyl bromides by using a cascade N-benzylation/C–H arylation reaction sequence. A series of pyrimido[5′,4′:4,5]pyrrolo[1,2-f]phenanthridines were successfully assembled via a domino process involving the palladium-catalyzed direct double C–H arylation reactions of 2,4,7-triarylpyrrolo[2,3-d]pyrimidines with o-bromoiodobenzenes.

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49

Zhou, Jing, Zhengtong Mao, Haokun Pan i Xingxian Zhang. "Pd-Catalyzed highly selective and direct ortho C–H arylation of pyrrolo[2,3-d]pyrimidine derivatives". Organic Chemistry Frontiers 7, nr 2 (2020): 324–28. http://dx.doi.org/10.1039/c9qo01312a.

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Pd-Catalyzed one-pot direct ortho C–H arylation of pyrrolo[2,3-d]pyrimidine derivatives is reported. This protocol provides a variety of biphenyl-containing pyrrolo[2,3-d]pyrimidines in good to excellent yields.

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Azam, Mohammed Afzal, Loganathan Dharanya, Charu Chandrakant Mehta i Sumit Sachdeva. "Synthesis and biological evaluation of some novel pyrazolopyrimidines incorporating a benzothiazole ring system". Acta Pharmaceutica 63, nr 1 (1.03.2013): 19–30. http://dx.doi.org/10.2478/acph-2013-0001.

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In the present study, a series of benzothiazol derivatives 3a-l containing pyrazolo[3,4-d]pyrimidine moiety at the second position were synthesized and characterized by analytical and spectral data. The compounds were tested for their in vitro antimicrobial activity. Compounds 1-(1,3-benzothiazol-2- yl)-3-methyl-4-phenyl-1H-pyrazolo[3,4-d]pyrimidine (3a), 1- (1,3-benzothiazol-2-yl)-4-(4-chlorophenyl)-3-methyl-1H-pyrazolo[ 3,4-d]pyrimidine (3d) and 1-(1,3-benzothiazol-2-yl)- 3-methyl-4-substituted phenyl-1H-pyrazolo[3,4-d]pyrimidines (3h-j) showed significant inhibitory activity against P. aeruginosa whereas compounds 1-(1,3-benzothiazol-2-yl)-4- (2-chlorophenyl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3b), 2-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin- 4-yl]phenol (3e), 1-(1,3-benzothiazol-2-yl)-4-(3,4-dimethoxyphenyl)- 3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3h), 4-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyri midin-4-yl]-N,N-dimethylaniline (3j) and 1-(1,3-benzothiazol- 2-yl)-3-methyl-4-[2-phenylvinyl]-1H-pyrazolo[3,4-d]pyrimidine (3k) were found to be active against C. albicans. Some of these synthesized compounds were evaluated for their in vivo acute toxicity, analgesic, anti-inflammatory, and ulcerogenic actions. The tested compound 4-[1-(1,3-benzothiazol- 2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-4-yl]-N, N-dimethylaniline (3j) exhibited maximum analgesic and anti-inflammatory activities. Compounds 1-(1,3-benzothiazol- -2-yl)-3-methyl-4-(3-nitrophenyl)-1H-pyrazolo[3,4-d]pyrimidine (3i) and 3j showed a significant gastrointestinal protection compared to the standard drug diclofenac sodium.

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