Статті в журналах: "Aryls(Heteroaryls) compound"

1

Stefanello, Felipe S., Jean C. B. Vieira, Juliane N. Araújo, Vitória B. Souza, Clarissa P. Frizzo, Marcos A. P. Martins, Nilo Zanatta, Bernardo A. Iglesias, and Helio G. Bonacorso. "Solution and Solid-State Optical Properties of Trifluoromethylated 5-(Alkyl/aryl/heteroaryl)-2-methyl-pyrazolo[1,5-a]pyrimidine System." Photochem 2, no. 2 (May 19, 2022): 345–57. http://dx.doi.org/10.3390/photochem2020024.

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This paper describes the photophysical properties of a series of seven selected examples of 5-(alkyl/aryl/heteroaryl)-2-methyl-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidines (3), which contain alkyl, aryl, and heteroaryl substituents attached to the scaffolds of 3. Given the electron-donor groups and -withdrawing groups, the optical absorption and emission in the solid state and solution showed interesting results. Absorption UV–Vis and fluorescence properties in several solvents of a pyrazolo[1,5-a]pyrimidines series were investigated, and all derivatives were absorbed in the ultraviolet region despite presenting higher quantum emission fluorescence yields in solution and moderate emission in the solid state. Moreover, the solid-state thermal stability of compounds 3a–g was assessed using thermogravimetric analysis. The thermal decomposition profile showed a single step with almost 100% mass loss for all compounds 3. Additionally, the values of T0.05 are considerably low (72–187 °C), especially for compound 3a (72 °C), indicating low thermal stability for this series of pyrazolo[1,5-a]pyrimidines.

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2

Shui, Hongling, Yuhong Zhong, Renshi Luo, Zhanyi Zhang, Jiuzhong Huang, Ping Yang, and Nianhua Luo. "Cyclometalated iridium complexes-catalyzed acceptorless dehydrogenative coupling reaction: construction of quinoline derivatives and evaluation of their antimicrobial activities." Beilstein Journal of Organic Chemistry 18 (October 27, 2022): 1507–17. http://dx.doi.org/10.3762/bjoc.18.159.

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The acceptorless dehydrogenative coupling (ADC) reaction is an efficient method for synthesizing quinoline and its derivatives. In this paper, various substituted quinolines were synthesized from 2-aminobenzyl alcohols and aryl/heteroaryl/alkyl secondary alcohols in one pot via a cyclometalated iridium-catalyzed ADC reaction. This method has some advantages, such as easy availability of raw materials, mild reaction conditions, wide range of substrates, and environmental friendliness which conforms to the principles of green chemistry. Furthermore, a gram-scale experiment with low catalyst loading offers the potential to access the aryl/heteroaryl quinolones in suitable amounts. In addition, the antibacterial and antifungal activities of the synthesized quinolines were evaluated in vitro, and the experimental results showed that the antibacterial activities of compounds 3ab, 3ad, and 3ah against Gram-positive bacteria and compound 3ck against C. albicans were better than the reference drug norfloxacin.

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3

Kalam, Sirisha, Rajyalaxmi I, and Olivia S. "Synthesis and In vitro P-Glycoprotein Inhibitory Activity of Novel 1,4-Dihydropyridine Derivatives." International Journal of Pharmaceutical Sciences and Nanotechnology 7, no. 3 (August 31, 2014): 2544–52. http://dx.doi.org/10.37285/ijpsn.2014.7.3.6.

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Анотація:

Two series of new symmetrical 4-aryl-2,6-dimethyl-3,5-bis-N-(aryl/heteroaryl)-carbamoyl-1,4-dihydropyridines (4a-f) and asymmetrical 4-aryl-2,6-dimethyl-3-N-(aryl/hetero-aryl)-carbamoyl-5-ethyl carboxylate-1,4-dihydro-pyridines (5a-f) have been synthesized by simple, economical and eco-friendly, modified Hantzsch reaction using N-aryl/heteroarylacetoacetamides (3a-c), ethylaceto-acetate (for asymmetric), arylaldehydes and urea in presence of catalytic amounts of LiBr/Iodine and by microwave irradiation methods. The newly synthesized compounds were characterized by physical and spectral data, and evaluated for their possible in vitro MDR reversal activity by everted sac method using verapamil as standard P-gp inhibitor and domperidone as the standard P-gp substrate. Amongst the compounds tested, compound 4f exhibited the highest in vitro P-gp inhibitory activity. It was found to be more potent than the standard verapamil.

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4

Marzo, Leyre, Ignacio Pérez, Francisco Yuste, José Alemán, and José Luis García Ruano. "A straightforward alkynylation of Li and Mg metalated heterocycles with sulfonylacetylenes." Chemical Communications 51, no. 2 (2015): 346–49. http://dx.doi.org/10.1039/c4cc07574a.

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Анотація:

Coupling of alkynyl moieties to heterocyclic rings, without using transition metals, can be easily performed by the reaction of aryl or heteroaryl sulfonylacetylenes with heteroaryl-Li compounds or their corresponding less reactive magnesium derivatives.

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5

Narayanaperumal, Senthil, Ricardo S. Schwab, Wystan K. O. Teixeira, and Danilo Yano de Albuquerque. "Recent Advances in the Synthesis of Enantiomerically Enriched Diaryl, Aryl Heteroaryl, and Diheteroaryl Alcohols through Addition of Organometallic Reagents to Carbonyl Compounds." Synthesis 52, no. 13 (March 16, 2020): 1855–73. http://dx.doi.org/10.1055/s-0039-1690847.

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Анотація:

Enantiomerically enriched diaryl, aryl heteroaryl, and diheteroaryl alcohols are an important family of compounds known for their biological properties. Moreover, these molecules are highly privileged scaffolds used as building blocks for the synthesis of pharmaceutically relevant products. This short review provides background on the enantioselective arylation and heteroarylation of carbonyl compounds, as well as, the most significant improvements in this field with special emphasis on the application of organometallic reagents.1 Introduction2 Background on the Enantioselective Synthesis of Diaryl, Aryl Heteroaryl, and Diheteroaryl Alcohols3 Organozinc Reagents4 Organolithium Reagents5 Grignard Reagents6 Organoaluminum Reagents7 Organotitanium Reagents8 Organobismuth Reagents9 Miscellaneous10 Conclusion

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6

Saritha, Rajendhiran, Sesuraj Babiola Annes, Subramanian Saravanan, and Subburethinam Ramesh. "Carbazole based Electron Donor Acceptor (EDA) catalysis for the synthesis of biaryl and aryl–heteroaryl compounds." Organic & Biomolecular Chemistry 18, no. 13 (2020): 2510–15. http://dx.doi.org/10.1039/d0ob00282h.

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7

Sitapara, Sachin M., Jignesh H. Pandya, and Chandankumar Pashavan. "An Efficient Synthesis of Novel Triazolo-pyrimidine Derivatives using Copper Catalyzed Click Chemistry (CuAAC) Approach." Asian Journal of Organic & Medicinal Chemistry 7, no. 2 (2022): 153–58. http://dx.doi.org/10.14233/ajomc.2022.ajomc-p378.

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Анотація:

To synthesize new chemical entities, we have a focus on the aryl or heteroaryl compounds. The current work also relates to the synthesis of pharmaceutical and medicinally active compositions containing these types of compounds and their vast application of treating a wide class of diseases i.e. anticancer, antibacterial, antifungal, antimalarial via administering substituted aryl or heteroaryl compounds. In this work, an efficient synthetic route is developed to explore a wide variety of 1H-1,2,3-triazol-1-yl-N- (4-phenylpyrimidin-2-yl)acetamide derivatives and convergent access a diverse array of triazolopyrimidine analogs via click chemistry approach. The structures elucidation was completed by using 1H & 13C NMR, FT-IR, mass spectroscopy, elemental analysis. The developed morpholino-pyrimidine derivatives were further utilized of a diverse range of their chemotherapeutic value.

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8

Gangadurai, Chinnakuzhanthai, Giri Teja Illa, and D. Srinivasa Reddy. "FeCl3-catalyzed oxidative decarboxylation of aryl/heteroaryl acetic acids: preparation of selected API impurities." Organic & Biomolecular Chemistry 18, no. 41 (2020): 8459–66. http://dx.doi.org/10.1039/d0ob01790f.

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Анотація:

An iron catalyzed one-pot, environmentally benign protocol for the oxidative decarboxylation of aryl/heteroaryl acetic acids to synthesize corresponding carbonyl compounds and five important API impurities is described.

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9

Malik, Ayesha, Nasir Rasool, Iram Kanwal, Muhammad Ali Hashmi, Ameer Fawad Zahoor, Gulraiz Ahmad, Ataf Ali Altaf, Syed Adnan Ali Shah, Sadia Sultan, and Zainul Amiruddin Zakaria. "Suzuki–Miyaura Reactions of (4-bromophenyl)-4,6-dichloropyrimidine through Commercially Available Palladium Catalyst: Synthesis, Optimization and Their Structural Aspects Identification through Computational Studies." Processes 8, no. 11 (October 23, 2020): 1342. http://dx.doi.org/10.3390/pr8111342.

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5-(4-bromophenyl)-4,6-dichloropyrimidine was arylated with several aryl/heteroaryl boronic acids via the Suzuki cross-coupling reaction by using Pd(0) catalyst to yield novel pyrimidine analogs (3a-h). It was optimized so that good yields were obtained when 5 mol % Pd(PPh3)4 was used along with K3PO4 and 1,4-Dioxane. Electron-rich boronic acids were succeeded to produce good yields of products. Density functional theory (DFT) calculations were also applied on these new compounds to analyze their reactivity descriptors and electronic and structural relationship. According to DFT studies, compound 3f is the most reactive one, while 3g is the most stable one. As per DFT studies, the hyperpolarizability (β) values of these compounds do not show them as very good non-linear optical (NLO) materials. Compound 3f has the highest β value among all the compounds under study but still it is not high enough to render it a potent NLO material.

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10

Saritha, Rajendhiran, Sesuraj Babiola Annes, Saravanan Subramanian, and Subburethinam Ramesh. "Correction: Carbazole based Electron Donor Acceptor (EDA) catalysis for the synthesis of biaryl and aryl–heteroaryl compounds." Organic & Biomolecular Chemistry 18, no. 15 (2020): 2962. http://dx.doi.org/10.1039/d0ob90043e.

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Correction for ‘Carbazole based Electron Donor Acceptor (EDA) catalysis for the synthesis of biaryl and aryl–heteroaryl compounds’ by Rajendhiran Saritha et al., Org. Biomol. Chem., 2020, DOI: 10.1039/d0ob00282h.

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11

Kartsev, Victor, Athina Geronikaki, Alexander Zubenko, Anthi Petrou, Marija Ivanov, Jasmina Glamočlija, Marina Sokovic, Lyudmila Divaeva, Anatolii Morkovnik, and Alexander Klimenko. "Synthesis and Antimicrobial Activity of New Heteroaryl(aryl) Thiazole Derivatives Molecular Docking Studies." Antibiotics 11, no. 10 (September 30, 2022): 1337. http://dx.doi.org/10.3390/antibiotics11101337.

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Herein, we report the design, synthesis, and evaluation of the antimicrobial activity of new heteroaryl (aryl) thiazole derivatives. The design was based on a molecular hybridization approach. The in vitro evaluation revealed that these compounds demonstrated moderate antibacterial activity. The best activity was achieved for compound 3, with MIC and MBC in the range of 0.23–0.7 and 0.47–0.94 mg/mL, respectively. Three compounds (2, 3, and 4) were tested against three resistant strains, namely methicillin resistant Staphylococcus aureus, P. aeruginosa, and E. coli, which showed higher potential than the reference drug ampicillin. Antifungal activity of the compounds was better with MIC and MFC in the range of 0.06–0.47 and 0.11–0.94 mg/mL, respectively. The best activity was observed for compound 9, with MIC at 0.06–0.23 mg/mL and MFC at 0.11–0.47 mg/mL. According to docking studies, the predicted inhibition of the E. coli MurB enzyme is a putative mechanism of the antibacterial activity of the compounds, while inhibition of 14a-lanosterol demethylase is probably the mechanism of their antifungal activity.

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12

Melford C Egbujor, Uchechukwu C Okoro, Samuel A Egu, Pius I Egwuatu, Florence U Eze, and Ifeanyi S Amasiatu. "Synthesis and Biological Evaluation of Alanine Derived Bioactive p-Toluenesulphonamide Analogs." International Journal of Research in Pharmaceutical Sciences 11, no. 4 (October 19, 2020): 6449–58. http://dx.doi.org/10.26452/ijrps.v11i4.3440.

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Sulphonamides and carboxamides have great pharmacological importance. The purpose of the study was to synthesize alanine-derived bioactive sulphonamides bearing carboxamides and evaluate their biological activities. The reaction of p-toluenesulphonyl chloride with L-alanine afforded compound 1, which was acetylated to obtain compound 2. The chlorination and ammonolysis of compound 2 gave the carboxamide backbone (3) which was coupled with aryl/heteroaryl halides to afford the hybrid compounds 4, 5 and 6. Structures were confirmed by FTIR, 1H-NMR, 13C-NMR spectra and elemental analytical data. The in vitro antimicrobial properties were determined by agar dilution, and the antioxidant properties were also investigated. Molecular docking interactions of the analogues were determined using PyRx. Compounds 4, 5 and 6 exhibited excellent in vitro antimicrobial properties in the range of 0.5-1.0mg/ml while compounds 1and 2 had half-maximal inhibitory concentration (IC50) of 1.11±0.15µg/ml and 1.12±0.13µg/ml respectively. For the molecular docking studies, compounds 5 and 6 displayed the best antitrypanosomal activity with binding affinities of -13.95 and -13.51kcal/mol respectively while compound 4 showed the highest in silico antimalarial activity having binding affinity of -11.95kcal/mol. All the alanine derived sulphonamides were observed to be potential antimicrobial, antioxidant, antitrypanosomal and antimalarial agents following the biological activities studies.

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13

Lopp, Margus, Eleana Lopušanskaja, Anne Paju, and Ivar Järving. "Synthesis of Cyclic 3-Aryl-Substituted 1,2-Dicarbonyl Compounds via Suzuki Cross-Coupling Reactions." Synthesis 50, no. 09 (February 12, 2018): 1883–90. http://dx.doi.org/10.1055/s-0036-1591543.

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Анотація:

A method for the synthesis of cyclic 3-aryl- and heteroaryl-substituted 1,2-dicarbonyl compounds with different ring sizes by using a Suzuki cross-coupling reaction between 3-halo-1,2-dicarbonyl compounds and arylboronic acids is developed. The 3-halo-1,2-dicarbonyl substrates are easily available from 1,2-dicarbonyl compounds. The method is versatile, affording good to high yields of the target compounds.

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14

Lan, Jihong, Rongxiang Chen, Fangfang Duo, Menghui Hu, and Xiaoyan Lu. "Visible-Light Photocatalytic Reduction of Aryl Halides as a Source of Aryl Radicals." Molecules 27, no. 17 (August 23, 2022): 5364. http://dx.doi.org/10.3390/molecules27175364.

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Анотація:

Aryl- and heteroaryl units are present in a wide variety of natural products, pharmaceuticals, and functional materials. The method for reduction of aryl halides with ubiquitous distribution is highly sought after for late-stage construction of various aromatic compounds. The visible-light-driven reduction of aryl halides to aryl radicals by electron transfer provides an efficient, simple, and environmentally friendly method for the construction of aromatic compounds. This review summarizes the recent progress in the generation of aryl radicals by visible-light-driven reduction of aryl halides with metal complexes, organic compounds, semiconductors as catalysts, and alkali-assisted reaction system. The ability and mechanism of reduction of aromatic halides in various visible light induced systems are summarized, intending to illustrate a comprehensive introduction of this research topic to the readers.

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15

Wang, Cuiying, Chang-Duo Yue, Jia Yuan, Jia-Lian Zheng, Ying Zhang, Hong Yu, Jian Chen, et al. "Synthesis of P-chiral phosphine compounds by palladium-catalyzed C–P coupling reactions." Chemical Communications 56, no. 79 (2020): 11775–78. http://dx.doi.org/10.1039/d0cc05340f.

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An efficient C–P coupling reactions of enantiopure tert-butylmethylphosphine-boranes with aryl and heteroaryl halides is developed by using Pd(OAc)₂/dppf as a catalyst, affording a series of P-chiral phosphines (up to 99% ee).

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16

Li, Yabo, Jingran Wang, Zhiwei Wang, Mengmeng Huang, Beiqi Yan, Xiuling Cui, Yusheng Wu, and Yangjie Wu. "Palladacycle-catalyzed Suzuki–Miyaura reaction of aryl/heteroaryl halides with MIDA boronates in EtOH/H2O or H2O." RSC Adv. 4, no. 68 (2014): 36262–66. http://dx.doi.org/10.1039/c4ra07486f.

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With good to excellent yields, a series of mono- or diheteroaryl compounds were synthesized via the palladacycle-catalyzed Suzuki–Miyaura reaction of various N-methyliminodiacetic acid (MIDA) boronates with aryl/heteroaryl halides in EtOH/H₂O or H₂O.

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17

Kutchin, Alexander V., Svetlana A. Rubtsova, Olga M. Lezina, Denis V. Sudarikov, Larisa L. Frolova, Irina V. Loginova, Alexey V. Popov, and Olga N. Grebyonkina. "Studies on oxidative transformations of thiols, sulfides and alcohols in the presence of chlorine dioxide." Pure and Applied Chemistry 89, no. 10 (September 26, 2017): 1379–401. http://dx.doi.org/10.1515/pac-2016-1209.

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AbstractOur recent studies on the chemical reactivity of chlorine dioxide in the reactions with sulfur and oxygen containing compounds are reviewed. A special attention is given to chlorine dioxide interaction with alkyl, aryl, heteroaryl, monoterpenyl thiols, sulfides and disulfides. The data on the oxidation of monoterpene alcohols and phenols are also presented. The directions of reactions depending on the structure of the compounds were identified.

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18

Knochel, Paul, Matthias A. Schade, Sebastian Bernhardt, Georg Manolikakes, Albrecht Metzger, Fabian M. Piller, Christoph J. Rohbogner, and Marc Mosrin. "Functionalization of heterocyclic compounds using polyfunctional magnesium and zinc reagents." Beilstein Journal of Organic Chemistry 7 (September 13, 2011): 1261–77. http://dx.doi.org/10.3762/bjoc.7.147.

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In this review we summarize the most important procedures for the preparation of functionalized organzinc and organomagnesium reagents. In addition, new methods for the preparation of polyfunctional aryl- and heteroaryl zinc- and magnesium compounds, as well as new Pd-catalyzed cross-coupling reactions, are reported herein. Experimental details are given for the most important reactions in the Supporting Information File 1 of this article.

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19

Begum, Shaheen, V. Anitha Kumari, S. K. Arifa Begum, M. Reddemma, K. Tejaswini, and K. Bharathi. "Synthesis and Evaluation of 1,2,4-Triazole Derivatives for Antioxidant, Anti-inflammatory, Cytotoxicity and QSAR Analysis." Asian Journal of Chemistry 35, no. 1 (December 27, 2022): 194–202. http://dx.doi.org/10.14233/ajchem.2023.26878.

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A series of novel 4-amino-5-substituted-1,2,4-triazole-3-thiol derivatives (B1-B18) were synthesized and characterized by spectral analysis. Equimolar portions of thiocarbohydrazide and different acids (substituted aryl/heteroaryl/aliphatic) were fused to synthesize the title compounds. The compounds were evaluated for cytotoxicity, in vitro anti-inflammatory activity and antioxidant activities. Cytotoxicity studies highlighted B4 (2,4-dichloro analog) as the potent cytotoxic molecule with IC50 value of 20.35 μM against MCF-7 cell line compared to cisplatin (IC50 = 12.06 μM). B4 (2,4-dichloro), B18 (oleayl) and B14 (2-hydroxy) showed significant membrane-stabilizing activity with IC50 values < 35 μM, whereas B11 (3,4-dimethoxy), B4 (2,4-dichloro) and B14 (2-hydroxy) displayed moderate proteinase inhibitory activity with IC50 values < 72 μM. Compounds possessing phenolic hydroxyl group (B12−B14) demonstrated an appreciable antioxidant activity in the studied antioxidant models. QSAR analysis revealed the important contribution of molecular connectivity, ionization potential and mass of the compounds for optimum cytotoxicity. Present results suggested compound B4 as a potential lead molecule to design novel and potent cytotoxic and anti-inflammatory agents.

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20

Bhatewara, Anjna, Srinivasa Rao Jetti, Tanuja Kadre, Pradeep Paliwal, and Shubha Jain. "Microwave-Assisted Synthesis and Biological Evaluation of Dihydropyrimidinone Derivatives as Anti-Inflammatory, Antibacterial, and Antifungal Agents." International Journal of Medicinal Chemistry 2013 (April 15, 2013): 1–5. http://dx.doi.org/10.1155/2013/197612.

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Анотація:

A simple protocol for the efficient preparation of aryl and heteroaryl substituted dihydropyrimidinone has been achieved via initial Knoevenagel, subsequent addition, and final cyclization of aldehyde, ethylcyanoacetate, and guanidine nitrate in the presence of piperidine as a catalyst in solvent-free under microwave irradiation. The synthesized compounds showed a good anti-inflammatory, antibacterial, and antifungal activity.

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21

Kumar, Dinesh, Gurpreet Singh, Pooja Sharma, Arem Qayum, Girish Mahajan, M. J. Mintoo, Shashank Kumar Singh, et al. "4-aryl/heteroaryl-4H-fused Pyrans as Anti-proliferative Agents: Design, Synthesis and Biological Evaluation." Anti-Cancer Agents in Medicinal Chemistry 18, no. 1 (March 16, 2018): 57–73. http://dx.doi.org/10.2174/1871520617666170918143911.

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Aims: The current study is focused on the design and synthesis of 4-aryl/heteroaryl-4H-fused pyrans as anti-proliferative agents. All the synthesized molecules were screened against a panel of human carcinoma cell lines. Description: Significant inhibition was exhibited by the compounds against HCT-116 (Colon) and PC-3 (Prostate) cell lines while A-549 (Lung) cell lines, MiaPaCa-2 (Pancreatic) cell lines and HL-60 (Leukemia Cancer) cell lines were almost resistant to the exposure of the test compounds. Compound FP-(v)n displayed noteworthy cytotoxicity towards HCT-116 malignant cells with the IC50 value of 0.67 µM. It induces apoptosis as revealed by several biological endpoints like apoptotic body formation, through DAPI staining, phase contrast microscopy and mitochondrial membrane potential loss. Moreover FP-(v)n is a potent apoptotic inducer confirmed by cell cycle arrest and ROS generation. The cell phase distribution studies indicate an augment from 4.94 % (control sample) to 39.68 % (sample treated with 1.5 µM compound FP-(v)n) in the apoptotic population. Compound FP-(v)n inhibits the tumor growth in Ehrlich ascites carcinoma (EAC), Ehrlich Tumor (ET, solid) and sarcoma-180 (solid) mice models. Additionally, it was established to be non-toxic at maximum tolerated dose of 1000 mg/kg in acute oral toxicity in Swiss-albino mice. Conclusion: The current study provides an insight into anti-cancer potential of FP-(v)n, which might be valuable in the treatment of tumor.

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22

Ahmad, Gulraiz, Nasir Rasool, Adeel Mubarik, Ameer Fawad Zahoor, Muhammad Ali Hashmi, Muhammad Zubair, Muhammad Bilal, Mohamed Hussien, Muhammad Saeed Akhtar, and Sajjad Haider. "Facile Synthesis of 5-Aryl-N-(pyrazin-2-yl)thiophene-2-carboxamides via Suzuki Cross-Coupling Reactions, Their Electronic and Nonlinear Optical Properties through DFT Calculations." Molecules 26, no. 23 (December 2, 2021): 7309. http://dx.doi.org/10.3390/molecules26237309.

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Анотація:

Synthesis of 5-aryl-N-(pyrazin-2-yl)thiophene-2-carboxamides (4a–4n) by a Suzuki cross-coupling reaction of 5-bromo-N-(pyrazin-2-yl)thiophene-2-carboxamide (3) with various aryl/heteroaryl boronic acids/pinacol esters was observed in this article. The intermediate compound 3 was prepared by condensation of pyrazin-2-amine (1) with 5-bromothiophene-2-carboxylic acid (2) mediated by TiCl4. The target pyrazine analogs (4a–4n) were confirmed by NMR and mass spectrometry. In DFT calculation of target molecules, several reactivity parameters like FMOs (EHOMO, ELUMO), HOMO–LUMO energy gap, electron affinity (A), ionization energy (I), electrophilicity index (ω), chemical softness (σ) and chemical hardness (η) were considered and discussed. Effect of various substituents was observed on values of the HOMO–LUMO energy gap and hyperpolarizability. The p-electronic delocalization extended over pyrazine, benzene and thiophene was examined in studying the NLO behavior. The chemical shifts of 1H NMR of all the synthesized compounds 4a–4n were calculated and compared with the experimental values.

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23

Zonjić, Iva, Lidija-Marija Tumir, Ivo Crnolatac, Filip Šupljika, Livio Racané, Sanja Tomić, and Marijana Radić Stojković. "Recognition of ATT Triplex and DNA:RNA Hybrid Structures by Benzothiazole Ligands." Biomolecules 12, no. 3 (February 27, 2022): 374. http://dx.doi.org/10.3390/biom12030374.

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Анотація:

Interactions of an array of nucleic acid structures with a small series of benzothiazole ligands (bis-benzothiazolyl-pyridines—group 1, 2-thienyl/2-benzothienyl-substituted 6-(2-imidazolinyl)benzothiazoles—group 2, and three 2-aryl/heteroaryl-substituted 6-(2-imidazolinyl)benzothiazoles—group 3) were screened by competition dialysis. Due to the involvement of DNA:RNA hybrids and triplex helices in many essential functions in cells, this study’s main aim is to detect benzothiazole-based moieties with selective binding or spectroscopic response to these nucleic structures compared to regular (non-hybrid) DNA and RNA duplexes and single-stranded forms. Complexes of nucleic acids and benzothiazoles, selected by this method, were characterized by UV/Vis, fluorescence and circular dichroism (CD) spectroscopy, isothermal titration calorimetry, and molecular modeling. Two compounds (1 and 6) from groups 1 and 2 demonstrated the highest affinities against 13 nucleic acid structures, while another compound (5) from group 2, despite lower affinities, yielded higher selectivity among studied compounds. Compound 1 significantly inhibited RNase H. Compound 6 could differentiate between B- (binding of 6 dimers inside minor groove) and A-type (intercalation) helices by an induced CD signal, while both 5 and 6 selectively stabilized ATT triplex in regard to AT duplex. Compound 3 induced strong condensation-like changes in CD spectra of AT-rich DNA sequences.

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24

Rocha, Inaiá O., Yuri G. Kappenberg, Wilian C. Rosa, Clarissa P. Frizzo, Nilo Zanatta, Marcos A. P. Martins, Isadora Tisoco, Bernardo A. Iglesias, and Helio G. Bonacorso. "Photophysical, photostability, and ROS generation properties of new trifluoromethylated quinoline-phenol Schiff bases." Beilstein Journal of Organic Chemistry 17 (December 1, 2021): 2799–811. http://dx.doi.org/10.3762/bjoc.17.191.

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Анотація:

A new series of ten examples of Schiff bases, namely (E)-2-(((2-alkyl(aryl/heteroaryl)-4-(trifluoromethyl)quinolin-6-yl)imino)methyl)phenols 3, was easily synthesized with yields of up to 91% from the reactions involving a series of 2-(R-substituted) 6-amino-4-(trifluoromethyl)quinolines 1 and 4(5)-R1-substituted salicylaldehydes 2 – in which alkyl/aryl/heteroaryl for 2-R-substituents are Me, Ph, 4-MeC6H4, 4-FC6H4, 4-NO2C6H4, and 2-furyl, and R1-substituents are 5-NEt2, 5-OCH3, 4-Br, and 4-NO2. Complementarily, the Schiff bases showed low to good quantum fluorescence yield values in CHCl3 (Φf = 0.12–0.80), DMSO (Φf = 0.20–0.75) and MeOH (Φf = 0.13–0.85). Higher values of Stokes shifts (SS) were observed in more polar solvents (DMSO; 65–150 nm and MeOH; 65–130 nm) than in CHCl3 (59–85 nm). Compounds 3 presented good stability under white-LED irradiation conditions and moderate ROS generation properties were observed.

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25

Poor Heravi, Mohammad Reza, and Marjan Ashori. "Boric Acid Catalyzed Convenient Synthesis of Benzimidazoles in Aqueous Media." Journal of Chemistry 2013 (2013): 1–5. http://dx.doi.org/10.1155/2013/496413.

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Анотація:

Synthesis of benzimidazoles has been developed by theo-phenylenediamine with aldehydes using boric acid an efficient catalyst under mild reaction conditions in aqueous media. The product is applicable to aryl and heteroaryl aldehydes. This reaction led to the formation of benzimidazoles new derivatives in good yields. The FT-IR,19F-NMR,1H-NMR,13C-NMR spectra and elemental analysis confirm the structure of compounds.

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26

K, Madhavi, and P. Sudeepthi. "Synthesis of Cyanoacetylated Derivatives of Some Heteroaryl Amines as Analgesic and Antioxidant Agents." International Journal of Pharmaceutical Sciences and Nanotechnology 5, no. 4 (February 28, 2013): 1879–84. http://dx.doi.org/10.37285/ijpsn.2012.5.4.8.

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Анотація:

There are several drugs in the clinical practice that contain the cyanoacetyl moiety. In the present study, we prepared cyanoacetylated derivatives of some aryl/hetero aryl amines by using a versatile cyanoacetylating agent, 1-cyanoacetyl-3,5-dimethylpyrazole. These compounds were evaluated for analgesic activity by the acetic acid induced writhing test. The compounds were also evaluated for antioxidant activity by reduction of DPPH, scavenging of nitric oxide, and iron-induced lipid peroxidation in rat brain homogenate. Among several compounds synthesized and evaluated, ethyl-2-(α-cyanoacetamido)-4,5-dimethylthiophene-3-carboxylate exhibited potent analgesic and antioxidant activity, which is comparable to the standard drug employed. These compounds have promising potential as potential analgesic and antioxidant agents.

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27

Poisson, Thomas, Maria Ivanova, Tatiana Besset, and Xavier Pannecoucke. "Palladium-Catalyzed Synthesis of Aryl and Heteroaryl Difluoromethylated Phosphonates." Synthesis 50, no. 04 (November 29, 2017): 778–84. http://dx.doi.org/10.1055/s-0036-1589140.

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Анотація:

We report the palladium-catalyzed introduction of the difluoromethylposphonate unit onto aryl and heteroaryl iodides under mild conditions. Using the CuCF2PO(OEt)2 species generated in situ, the method allows the functionalization of various otherwise reluctant substrates. In addition, this reaction permits the formation of CF2PO(OEt)2-containing heterocycles, an important class of compounds. This process broadens the current toolbox of methods available to construct CF2PO(OEt)2-containing molecules.

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28

Bogdanov, Milen G., Meglena I. Kandinska, Darina B. Dimitrova, Blagovesta T. Gocheva, and Mariana D. Palamareva. "Preliminary Evaluation of Antimicrobial Activity of Diastereomeric cis/trans-3-Aryl(Heteroaryl)-3,4-dihydroisocoumarin-4-carboxylic Acids." Zeitschrift für Naturforschung C 62, no. 7-8 (August 1, 2007): 477–82. http://dx.doi.org/10.1515/znc-2007-7-804.

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Анотація:

Preliminary differentiating screening of the antibacterial and antifungal activity of a series of diastereomeric cis/trans-3-aryl(heteroaryl)-3,4-dihydroisocoumarin-4-carboxylic acids (3a- i) was performed by the agar diffusion method against twelve microorganism strains of different taxonomic groups. S. aureus and A. niger were the most sensitive strains to the antibiotic effect of the tested compounds, both inhibited by 10 of 12 compounds. The most potent antibacterial agent was cis-3-phenyl-3,4-dihydroisocoumarin-4-carboxylic acid (cis-3a), exhibiting activity against all seven bacterial test strains

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29

Mathew, Vinod, J. Keshavayya, and V. P. Vaidya. "Synthesis, Characterization and Pharmacological Activities of 3,6-Disubstituted-1,2,4-triazolo [3,4-b]-1,3,4-thiadiazoles and their Dihydro Analogues." E-Journal of Chemistry 4, no. 3 (2007): 320–42. http://dx.doi.org/10.1155/2007/605058.

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Анотація:

4-Amino-5-aryl/heteroaryl substituted-3-mercapto-1,2,4-triazoles 3(a-d) were prepared from the corresponding aromatic carboxylic acids through a multi-step sequence. Compounds 3(a-d) were made to react with various aromatic/hetero aromatic acids and hetero aromatic aldehydes to give 3,6-disubstituted-1,2,4-triazolo [3,4-b]-1,3,4-thiadizoles and 3,6-disubstituted-5,6-dihydro-1,2,4-triazolo [3,4-b]-1,3,4-thiadizoles respectively. Elemental analysis, IR,1H NMR and mass spectral data elucidated the structures of all newly synthesized compounds. Synthesized compounds are studied for their antibacterial, antifungal, anti-inflammatory and analgesic activities. Some of the tested compounds showed significant pharmacological activities.

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30

Hurtová, Martina, David Biedermann, Zuzana Osifová, Josef Cvačka, Kateřina Valentová, and Vladimír Křen. "Preparation of Synthetic and Natural Derivatives of Flavonoids Using Suzuki–Miyaura Cross-Coupling Reaction." Molecules 27, no. 3 (January 31, 2022): 967. http://dx.doi.org/10.3390/molecules27030967.

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Анотація:

Herein, we report the use of the Suzuki–Miyaura cross-coupling reaction for the preparation of a library of synthetic derivatives of flavonoids for biological activity assays. We have investigated the reactivity of halogenated flavonoids with aryl boronates and with boronyl flavonoids. This reaction was used to prepare new synthetic derivatives of flavonoids substituted at C-8 with aryl, heteroaryl, alkyl, and boronate substituents. The formation of flavonoid boronate enabled a cross-coupling reaction with halogenated flavones yielding biflavonoids connected at C-8. This method was used for the preparation of natural compounds including C-8 prenylated compounds, such as sinoflavonoid NB. Flavonoid boronates were used for the preparation of rare C-8 hydroxyflavonoids (natural flavonoids gossypetin and hypolaetin). A series of previously unknown derivatives of quercetin and luteolin were prepared and fully characterized.

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31

Averin, Alexei D., Anton S. Abel, Olga K. Grigorova, Gennadij V. Latyshev, Yury N. Kotovshchikov, Alexander Yu Mitrofanov, Alla Bessmertnykh-Lemeune, and Irina P. Beletskaya. "Recent achievements in copper catalysis for C–N bond formation." Pure and Applied Chemistry 92, no. 8 (September 25, 2020): 1181–99. http://dx.doi.org/10.1515/pac-2020-0301.

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Анотація:

AbstractA mini-review describes the development of the catalysis by Cu(I) complexes aimed at the formation of C–N bond at the Lomonosov MSU during 2010s. The main approach employs the amination of aryl and heteroaryl halides with the amines and polyamines, in this direction a great versatility of starting compounds was achieved: adamantane-containing amines, linear diamines, oxadiamines and polyamines, various aryl iodides and bromides, derivatives of pyridine, and quinoline were used for this purpose. In more peculiar cases, the copper catalysis was used for steroids transformations, including vinylation of azoles, wide-spread “click” reactions for the conjugate syntheses, and successful heterogenezation of the copper catalysts were also undertaken.

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32

Baraldi, Pier G., Roberta Budriesi, Barbara Cacciari, Alberto Chiarini, Laura Garuti, Giuseppe Giovanninetti, Alberto Leoni, and Marinella Roberti. "Synthesis and Calcium Antagonist Activity of Dialkyl 1,4-Dihydro-2,6-dimethyl-4-(nitrogenous heteroaryl)-3,5-pyridine Dicarboxylates." Collection of Czechoslovak Chemical Communications 57, no. 1 (1992): 169–78. http://dx.doi.org/10.1135/cccc19920169.

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Анотація:

A new series of 4-(nitrogenous heteroaryl)-1,4-dihydropyridine antagonists II - XVI were synthesized and screened for inotropic, chronotropic and calcium antagonist properties, in order to evaluate the effect on pharmacological activity of replacement of the 4-aryl group of nifedipine-like drugs by heterocyclic moieties, such as quinoline, indole, carbazole and pyrazole. The most potent bradycardic compounds of the series (VIII - X, XII and XIII) elicited weak calcium antagonist activity and were stronger negative inotropic.

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33

Dhanawat, Meenakshi, Sumeet Gupta, Rina Das, and Dinesh Kumar Mehta. "Assessing the affinity of oxazolidinedione/hydantoin derivatives for the human 5HT1A/2A receptor through homology modeling and docking studies." Journal of University of Shanghai for Science and Technology 23, no. 09 (September 4, 2021): 46–66. http://dx.doi.org/10.51201/jusst/21/09505.

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Анотація:

A flexible docking of a series of heteroaryl compounds to the binding site of a model of human 5-HT1A/2A receptor was exercised using GLIDE docking methods. The resultant docking scores were used to correlate the in vivo affinity data. The GLIDE docking algorithm when used with a homology model of 5HT1A/2A was based on β2- adrenergic receptor template. The influence of structure and hydrophobic properties of aryl moiety on binding affinities was discussed and a model for ligand binding in the hydrophobic part of the binding site was proposed.

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34

Katritzky, Alan R., Jianqing Li, Christian V. Stevens, and David J. Ager. "AN ALTERNATIVE SYNTHESIS OF ARYL AND HETEROARYL BROMIDES FROM ACTIVATED ARYL HYDROXY COMPOUNDS." Organic Preparations and Procedures International 26, no. 4 (August 1994): 439–44. http://dx.doi.org/10.1080/00304949409458034.

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35

Mosallanezhad, Asiyeh, and Hamzeh Kiyani. "Green Synthesis of 3-Substituted-4-arylmethylideneisoxazol-5(4H)-one Derivatives Catalyzed by Salicylic Acid." Current Organocatalysis 6, no. 1 (April 24, 2019): 28–35. http://dx.doi.org/10.2174/2213337206666190214161332.

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Анотація:

Background: 4-Arylmethylideneisoxazol-5(4H)-ones are a class of organic compounds with a variety of applications in the agriculture, filter dyes, photonic devices, and pharmaceutical industries. They are also used as synthetic precursors for the synthesis of other organic compounds. As a result, efforts are being made to search new and available catalyst and green methods toward their synthesis. Objective: The aim of this work is to investigate the catalytic activity of salicylic acid as an inexpensive, easy to handle, and safe catalyst to synthesis of some derivatives of isoxazole-5(4H)-ones in water medium. Methods: To aqueous solution of equal amounts of aryl/heteroaryl aldehydes, β-ketoesters, and hydroxylamine hydrochloride; salicylic acid (15 mol%) was added and the reaction mixture was stirred at room temperature for a specified periods. The precipitated product was filtered and washed with water to obtain 3-substituted-4-arylmethylideneisoxazol-5(4H)-ones. The reaction conditions were also optimized and extended to synthesis other isoxazol-5(4H)-ones. Results: The salicylic acid is found to possess acceptable catalytic activity for the promotion of three-component cyclocondensation of aryl/heteroaryl aldehydes, β-ketoesters, and hydroxylamine hydrochloride. The three-component reaction led to construction of 3-substituted-4-arylmethylideneisoxazol- 5(4H)-ones in good to high isolated reaction yields. Conclusion: The efficient and environmental friendliness procedure for the synthesis of isoxazol- 5(4H)-ones is introduced. The reaction also carried out smoothly in water as a cost-effective, simple, green, and non-toxic solvent at room temperature without using heating, microwave, and ultrasound sources.

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36

Błocka, Aleksandra, and Wojciech Chaładaj. "Tandem Pd-Catalyzed Cyclization/Coupling of Non-Terminal Acetylenic Activated Methylenes with (Hetero)Aryl Bromides." Molecules 27, no. 3 (January 19, 2022): 630. http://dx.doi.org/10.3390/molecules27030630.

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Анотація:

We report a new method for a tandem Pd-catalyzed intramolecular addition of active methylene compounds to internal alkynes followed by coupling with aryl and heteroaryl bromides. Highly substituted vinylidenecyclopentanes were obtained with good yields, complete selectivity, and excellent functional group tolerance. A plausible mechanism, supported by DFT calculations, involves the oxidative addition of bromoarene to Pd(0), followed by cyclization and reductive elimination. The excellent regio- and stereoselectivity arises from the 5-exo-dig intramolecular addition of the enol form of the substrate to alkyne activated by the π-acidic Pd(II) center, postulated as the rate-determining step.

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37

Nauš, Petr, Martin Kuchař, and Michal Hocek. "Cytostatic and Antiviral 6-Arylpurine Ribonucleosides IX. Synthesis and Evaluation of 6-Substituted 3-Deazapurine Ribonucleosides." Collection of Czechoslovak Chemical Communications 73, no. 5 (2008): 665–78. http://dx.doi.org/10.1135/cccc20080665.

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Анотація:

A series of 3-deazapurine ribonucleosides 5a-5l bearing diverse C-substituents (alkyl, aryl and heteroaryl) in the position 6 were prepared by Pd-catalyzed cross-coupling reactions of either free 6-chloro-3-deazapurine ribonucleoside 4 or its acetyl protected congener 3 followed by deprotection. An improved synthesis of the starting 4-chloro-1-(2,3,5-tri-O-acetyl-β-D-ribofuranosyl)-1H-imidazo[4,5-c]pyridine (3) was developed by the application of Vorbrüggen glycosylation of silylated nucleobase with 1,2,3,5-tetra-O-acetyl-β-D-ribofuranose (2). None of compounds 5a-5l showed any considerable cytostatic or antiviral activity.

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38

Sengmany, Stéphane, Eric Léonel, Rima Rahil, and Erwan Le Gall. "Nickel-Catalyzed Electrochemical Reductive Homocouplings of Aryl and Heteroaryl Halides: A Useful Route to Symmetrical Biaryls." Synthesis 50, no. 01 (September 12, 2017): 146–54. http://dx.doi.org/10.1055/s-0036-1589100.

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Анотація:

Due to their widespread presence in functional materials and pharmaceuticals, biaryls are of fundamental importance in organic chemistry. Methods for the synthesis of symmetrical biaryls generally involve both metallic reduction and transition-metal catalysis. In this work, we show that electroreduction can also constitute a very relevant way to achieve the nickel-catalyzed reductive synthesis of symmetrical biaryl compounds. Therefore, it is demonstrated that both aryl and heteroaryl halides undergo reductive coupling to furnish the corresponding symmetrical biaryls in fair to excellent yields. Reactions are performed under very mild conditions thus ensuring important functional group tolerance.

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39

Mahran, Mona, Samia William, Fatem Ramzy, and Amira Sembel. "Synthesis and in vitro Evaluation of New Benzothiazole Derivatives as Schistosomicidal Agents." Molecules 12, no. 3 (March 26, 2007): 622–33. http://dx.doi.org/10.3390/12030622.

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Анотація:

A series of benzothiazol-2-yl-dithiocarbamates 3a-d along with their copper complexes 4a-c were synthesized via the reaction of suitable alkyl, aralkyl or heteroaryl halides with the sodium salt of benzothiazol-2-yl-dithiocarbamic acid, followed by complexation with copper sulphate. N-(4-Acetyl-5-aryl-4,5-dihydro-1,3,4-thiadiazol-2-yl)-N-benzothiazol-2-yl-acetamides 7a-c were synthesized by cyclization of the appropriate thiosemicarbazones 6a-c in acetic anhydride. Selected compounds were screened for in vitro schistosomicidal activity against Schistosoma mansoni at three different dosage levels (10, 50 and 100 μg/ mL). Three of these products, 4a-c, showed schistosomicidal activity similar to praziquantel, with 100% worm mortality at 10 μg/mL. These compounds would constitute a new class of potent schistosomicidal agents.

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40

Omara, Mariam, Mohamed Hagras, Mohamed M. Elsebaie, Nader S. Abutaleb, Hanzada T. Nour El-Din, Maria O. Mekhail, Ahmed S. Attia, Mohamed N. Seleem, Marwa T. Sarg, and Abdelrahman S. Mayhoub. "Exploring novel aryl/heteroaryl-isosteres of phenylthiazole against multidrug-resistant bacteria." RSC Advances 13, no. 29 (2023): 19695–709. http://dx.doi.org/10.1039/d3ra02778c.

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Анотація:

Twenty-three compounds of novel phenylthiazole derivatives were synthesized utilizing the Suzuki coupling reaction. Antibacterial activity in an in vivo model against MRSA USA300 was evaluated, as it reduced the burden of MRSA USA300 in skin-infected mice.

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41

Dharuman, Suresh, Miranda J. Wallace, Stephanie M. Reeve, Jürgen B. Bulitta, and Richard E. Lee. "Synthesis and Structure–Activity Relationship of Thioacetamide-Triazoles against Escherichia coli." Molecules 27, no. 5 (February 24, 2022): 1518. http://dx.doi.org/10.3390/molecules27051518.

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Анотація:

Infections due to Gram-negative bacteria are increasingly dangerous due to the spread of multi-drug resistant strains, emphasizing the urgent need for new antibiotics with alternative modes of action. We have previously identified a novel class of antibacterial agents, thioacetamide-triazoles, using an antifolate targeted screen and determined their mode of action which is dependent on activation by cysteine synthase A. Herein, we report a detailed examination of the anti-E. coli structure–activity relationship of the thioacetamide-triazoles. Analogs of the initial hit compounds were synthesized to study the contribution of the aryl, thioacetamide, and triazole sections. A clear structure–activity relationship was observed generating compounds with excellent inhibition values. Substitutions to the aryl ring were generally best tolerated, including the introduction of thiazole and pyridine heteroaryl systems. Substitutions to the central thioacetamide linker section were more nuanced; the introduction of a methyl branch to the thioacetamide linker substantially decreased antibacterial activity, but the isomeric propionamide and N-benzamide systems retained activity. Changes to the triazole portion of the molecule dramatically decreased the antibacterial activity, further indicating that 1,2,3-triazole is critical for potency. From these studies, we have identified new lead compounds with desirable in-vitro ADME properties and in-vivo pharmacokinetic properties.

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42

Sechi, Mario, Luciano Sannia, Fabrizio Carta, Michele Palomba, Roberto Dallocchio, Alessandro Dessì, Massimiliano Derudas, Zahrah Zawahir та Nouri Neamati. "Design of Novel Bioisosteres of β-Diketo Acid Inhibitors of HIV-1 Integrase". Antiviral Chemistry and Chemotherapy 16, № 1 (лютий 2005): 41–61. http://dx.doi.org/10.1177/095632020501600105.

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Анотація:

HIV-1 integrase (IN) is an attractive and validated target for the development of novel therapeutics against AIDS. Significant efforts have been devoted to the identification of IN inhibitors using various methods. In this context, through virtual screening of the NCI database and structure-based drug design strategies, we identified several pharmacophoric fragments and incorporated them on various aromatic or heteroaromatic rings. In addition, we designed and synthesized a series of 5-aryl(heteroaryl)-isoxazole-3-carboxylic acids as biological isosteric analogues of β-diketo acid containing inhibitors of HIV-1 IN and their derivatives. Further computational docking studies were performed to investigate the mode of interactions of the most active ligands with the IN active site. Results suggested that some of the tested compounds could be considered as lead compounds and suitable for further optimization.

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43

Ghorab, Mostafa M., Mansour S. Al-Said, and Reem K. Arafa. "Design, Synthesis and Potential Anti-Proliferative Activity of Some Novel 4-Aminoquinoline Derivatives." Acta Pharmaceutica 64, no. 3 (September 1, 2014): 285–97. http://dx.doi.org/10.2478/acph-2014-0030.

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Анотація:

Abstract Novel nineteen compounds based on a 4-aminoquinoline scaffold were designed and synthesized as potential antiproliferative agents. The new compounds were N-substituted at the 4-position by aryl or heteroaryl (1-9), quinolin- 3-yl (10), 2-methylquinolin-3-yl (11), thiazol-2-yl (12), and dapsone moieties (13, 14 and 18). Bis-compounds 15, 16 and 19 were also synthesized to assess their biological activity. All the newly synthesized comounds were tested for in vitro antiproliferative activity against the MCF-7 breast cancer cell line. Seventeen of the novel compounds showed higher activity than the reference drug doxorubicin. The corresponding 7-(trifluoromethyl)-N-(3,4,5-trimethoxyphenyl)quinolin-4- amine 1, N-(7-(trifluoromethyl)quinolin-4-yl)quinolin- 3- amine (10), 2-methyl-N-(7-trifluorome-thyl)quinolin-4-yl) quinolin-3-amine (11) and N-(4-(4-aminophenylsulfonyl) phenyl)-7-chloroquinolin-4-amine (13) were almost twice to thrice as potent as doxorubicin. Biological screening of the tested compounds could offer an encouraging framework in this field that may lead to the discovery of potent anticancer agents.

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44

KATRITZKY, A. R., J. LI, C. V. STEVENS, and D. J. AGER. "ChemInform Abstract: An Alternative Synthesis of Aryl and Heteroaryl Bromides from Activated Aryl Hydroxy Compounds." ChemInform 26, no. 5 (August 18, 2010): no. http://dx.doi.org/10.1002/chin.199505089.

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45

Arasavelli, Ananda Mohan, Ganapavarapu Veera Raghava Sharma, and Siddaiah Vidavalur. "Design, synthesis, and anticancer activity of novel aryl/heteroaryl chalcone derivatives." Heterocyclic Communications 22, no. 1 (February 1, 2016): 1–5. http://dx.doi.org/10.1515/hc-2015-0271.

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Анотація:

AbstractA new series of chalcones 5a–l were synthesized and evaluated for in vitro antiproliferative activity against human colon cancer cell lines. The synthesis of the key intermediate compounds 3a–d was achieved by tetrakis(triphenylphosphine) palladium(II) mediated Suzuki cross coupling reaction. Chalcone 5a shows superior anticancer activity with IC50 value of 21.0 μg/mL compared to the IC50 value of the reference drug doxorubicin at 21.65 μg/mL.

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46

Ahmad, Sana, Suvendu Sekhar Dey, Bernard Jousseaume, and Thierry Toupance. "Linear or cross-shaped di(cyclopentadienyltitanium) compounds with aryl or heteroaryl spacers." Dalton Trans. 40, no. 2 (2011): 457–62. http://dx.doi.org/10.1039/c0dt01060j.

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47

Sutherland, Hamish S., Peter J. Choi, Guo-Liang Lu, Anna C. Giddens, Amy S. T. Tong, Scott G. Franzblau, Christopher B. Cooper, Brian D. Palmer, and William A. Denny. "Synthesis and Structure–Activity Relationships for the Anti-Mycobacterial Activity of 3-Phenyl-N-(Pyridin-2-ylmethyl)Pyrazolo[1,5-a]Pyrimidin-7-Amines." Pharmaceuticals 15, no. 9 (September 8, 2022): 1125. http://dx.doi.org/10.3390/ph15091125.

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Анотація:

Pyrazolo[1,5-a]pyrimidines have been reported as potent inhibitors of mycobacterial ATP synthase for the treatment of Mycobacterium tuberculosis (M.tb). In this work, we report the design and synthesis of approximately 70 novel 3,5-diphenyl-N-(pyridin-2-ylmethyl)pyrazolo[1,5-a]pyrimidin-7-amines and their comprehensive structure–activity relationship studies. The most effective pyrazolo[1,5-a]pyrimidin-7-amine analogues contained a 3-(4-fluoro)phenyl group, together with a variety of 5-alkyl, 5-aryl and 5-heteroaryl substituents. A range of substituted 7-(2-pyridylmethylamine) derivatives were also active. Some of these compounds exhibited potent in vitro M.tb growth inhibition, low hERG liability and good mouse/human liver microsomal stabilities, highlighting their potential as inhibitors of M.tb.

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48

Micheletti, Gabriele, and Carla Boga. "Nucleophile/Electrophile Combinations in Aromatic Substitution: From Wheland to Wheland–Meisenheimer Intermediates Using Strongly Activated Arenes." Synthesis 49, no. 15 (July 13, 2017): 3347–56. http://dx.doi.org/10.1055/s-0036-1588490.

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Анотація:

This short review provides an overview on the interaction between 1,3,5-triaminobenzene derivatives and different kinds of electrophiles. Due to the ambident reactivity of these nucleophiles (i.e., at the nitrogen atom of the substituents and at the aromatic carbon atom) different compounds can be obtained. Particular attention is devoted to the detection, isolation, and characterization of covalent intermediates of aromatic substitution, starting from Wheland intermediates until the first detection and characterization of Wheland–Meisenheimer intermediates.1 Introduction2 Reactions between 1,3,5-Triaminobenzene Derivatives and Charged Electrophiles2.1 The Proton as an Electrophile2.2 Arenediazonium Salts as Electrophiles3 Reactions between 1,3,5-Triaminobenzene Derivatives and Neutral Electrophiles3.1 Alkyl Halides as Electrophiles3.2 Acyl Halides and Sulfonyl Chlorides as Electrophiles3.3 Aryl Halides and Heteroaryl Halides as Electrophiles3.4 Polynitroheteroaromatics as Electrophiles4 Conclusion

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49

Ameur Messaoud, Mohamed Yacine Ameur, Ghenia Bentabed-Ababsa, Ziad Fajloun, Monzer Hamze, Yury S. Halauko, Oleg A. Ivashkevich, Vadim E. Matulis, Thierry Roisnel, Vincent Dorcet, and Florence Mongin. "Deprotometalation-Iodolysis and Direct Iodination of 1-Arylated 7-Azaindoles: Reactivity Studies and Molecule Properties." Molecules 26, no. 20 (October 19, 2021): 6314. http://dx.doi.org/10.3390/molecules26206314.

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Анотація:

Five protocols were first compared for the copper-catalyzed C-N bond formation between 7-azaindole and aryl/heteroaryl iodides/bromides. The 1-arylated 7-azaindoles thus obtained were subjected to deprotometalation-iodolysis sequences using lithium 2,2,6,6-tetramethylpiperidide as the base and the corresponding zinc diamide as an in situ trap. The reactivity of the substrate was discussed in light of the calculated atomic charges and the pKa values. The behavior of the 1-arylated 7-azaindoles in direct iodination was then studied, and the results explained by considering the HOMO orbital coefficients and the atomic charges. Finally, some of the iodides generated, generally original, were involved in the N-arylation of indole. While crystallographic data were collected for fifteen of the synthesized compounds, biological properties (antimicrobial, antifungal and antioxidant activity) were evaluated for others.

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Wunderlich, Stefan H, and Paul Knochel. "Aluminum Bases for the Highly Chemoselective Preparation of Aryl and Heteroaryl Aluminum Compounds." Angewandte Chemie International Edition 48, no. 8 (February 9, 2009): 1501–4. http://dx.doi.org/10.1002/anie.200804966.

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