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Journal articles on the topic 'Morpholines – chemical synthesis'

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Published: 4 June 2021
Last updated: 1 February 2022

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1

Reddy, B. Jayachandra, and M. C. Somasekhara Reddy. "Ultrasonicated Synthesis ofN-Benzyl-2,3-substituted Morpholines, via the Mitsunobu Diol Cyclisation." E-Journal of Chemistry 7, no. 4 (2010): 1184–89. http://dx.doi.org/10.1155/2010/931015.

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A facile five step synthesis ofN-benzyl-2,3-substituted morpholines (i-iii) was performed. The key steps were microwave assisted Friedel-crafts acylation and diol cyclization carried out via an ultra sonication of Mitsunobu reaction using DEAD (diethylazodicarboxylate), TPP in THF for 1 h. The morpholine products were generated as diasteriomers (iiandiii) which has been separated by the column chromatography to good yield. The structure of compounds (i-iii) has been characterized by the spectral and chemical studies.
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2

Magerramov, A. M., M. N. Magerramov, Kh A. Makhmudova, and G. I. Alizade. "Synthesis of N-Substituted Oxazolidines and Morpholines." Russian Journal of Applied Chemistry 78, no. 8 (August 2005): 1301–5. http://dx.doi.org/10.1007/s11167-005-0502-x.

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3

Beng, Timothy K., Abdikani Omar Farah, and Victoria Shearer. "Modular synthesis and transition metal-free alkynylation/alkenylation of Castagnoli–Cushman-derived N,O- and N,S-heterocyclic vinyl chlorides." RSC Advances 10, no. 61 (2020): 37153–60. http://dx.doi.org/10.1039/d0ra06619b.

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A functional group-tolerant and transition metal-free coupling of novel N,O- and N,S-heterocyclic vinyl chlorides, which affords fully carbosubstituted dihydro-1,4-oxazines/thiazines as well as bicyclic morpholines, is described.
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4

Cera, Gianpiero, Michel Chiarucci, and Marco Bandini. "Accessing chemical diversity by stereoselective gold-catalyzed manipulation of allylic and propargylic alcohols." Pure and Applied Chemistry 84, no. 8 (February 3, 2012): 1673–84. http://dx.doi.org/10.1351/pac-con-11-09-05.

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The combined use of asymmetric Au(I) catalysis with allylic as well as propargylic alcohols proved to be a competent synthetic tool, toward the realization of complex molecular organic architectures in a stereochemically defined manner. In particular, allylic alcohols have been utilized as alkylating agents in the synthesis of tetrahydrocarbazoles/carbolines and morpholines by means of new C–C and C–X bond-forming processes. Analogously, the direct activation of indole-propargylic alcohols with cationic Au complexes opened a direct access to tetracyclic fused indolines in a highly stereoselective manner.
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5

Rasulov, Ch K., A. G. Azizov, F. A. Nabiev, S. T. Rustamov, and A. S. Askerova. "Synthesis of N-[2-hydroxy-4(5)-methyl- and -5-(methylcyclohexyl)benzyl]morpholines as antioxidants for transformer oils." Russian Journal of Applied Chemistry 83, no. 12 (December 2010): 2140–43. http://dx.doi.org/10.1134/s107042721012013x.

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6

Journal, Baghdad Science. "Synthesis, Characterization and Study the Biological Activity of New Morpholine Derivative." Baghdad Science Journal 12, no. 4 (December 6, 2015): 761–73. http://dx.doi.org/10.21123/bsj.12.4.761-773.

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A new series of morpholine derivative were prepared by reacting the morpholine with ethyl chloro acetate in the presence triethylamine as an catalyst and benzene as a solvent gave the ethyl morpholin-4-ylacetate reaction with hydrazine hydrate and ethanol as a solvent gave the 2-(morpholin-4-yl)acetohydrazide gave series of Schiff base were prepared by reacting 2-(morpholin-4- yl)acetohydrazide with different aromatic aldehydes and ketons . The new series of (3-9 )were synthesis by reaction of Schiff base (10-14) with chloroacetyl chloride, triethyl amine as an catalyst and 1,4dioxane as a solvent .The chemical structures of the synthesis compound were identified by spectral methods their [ IR ,1H-NMR and 13C-NMR ].The synthesised compounds were screened for antibacterial activity and antifungal activity promising by disc diffusion method by measuring the zone of inhibition and the results were compared to standard drugs ciprofloxacin .
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7

D’hooghe, Matthias, Stijn Dekeukeleire, Erika Leemans, and Norbert De Kimpe. "Use of functionalized β-lactams as building blocks in heterocyclic chemistry." Pure and Applied Chemistry 82, no. 9 (June 4, 2010): 1749–59. http://dx.doi.org/10.1351/pac-con-09-09-39.

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β-Lactams represent flexible building blocks suitable for the preparation of a large variety of nitrogen-containing target compounds. In the present study, the formerly neglected synthetic potential of 4-haloalkyl-β-lactams has been elaborated in detail with a focus on the preparation of different mono- and bicyclic heterocycles. A first approach involved ring transformations of these halogenated building blocks toward stereodefined aziridines, azetidines, pyrrolidines, and piperidines via intermediate aziridinium or azetidinium ions. In a second part, novel and stereoselective entries into 1,4- and 3,4-fused bicyclic β-lactams were developed through either a radical or an ionic cyclization protocol. Furthermore, the ring enlargement of halogenated β-lactams into functionalized mono- and bicyclic pyrrolidin-2-ones was established as the aza-analog of the cyclobutylmethylcarbenium ion to cyclopentylcarbenium ion rearrangement. Finally, chiral versions toward azetidin-2-ones and ring transformation products were elaborated, involving the synthesis of 3(S)-alkoxy-4(S)-[1(S)-chloroethyl]azetidin-2-ones and the preparation of bicyclic β-lactams annelated to piperazines, morpholines, and diazepanes.
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8

Hermecz, István, Andrea Sánta-Csutor, Csaba Gönczi, Gergely Héja, Éva Csikós, Kálmán Simon, Ágota Smelkó-Esek, and Benjámin Podányi. "Chemical development of the vasopressin receptor 2 antagonist SR-121463." Pure and Applied Chemistry 73, no. 9 (September 1, 2001): 1401–9. http://dx.doi.org/10.1351/pac200173091401.

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A facile convergent total synthesis of the selective, potent, and orally active V2 non-peptide antagonist, SR-121463, was developed by modification of the discovery route. One of the late intermediates, the sulfonyl chloride 1, was synthesized from 3-hydroxybenzoic acid (19) by regioselective sulfonation, O-methylation and amidation in four steps. Another late intermediate, indolin-2-one 2, was prepared from p-phenetidine (8) through the indolin-2-one 16, where the cyclohexanone moiety of 27 was introduced into the active 3-methylene group of 16 by sequential transformation using methyl acrylate and KOtBu. After formation of the cyclic ketal moiety of 13, its ring-opening was achieved by using NaBH4 in the presence of CCl3COOH. The morpholino group in 2 was introduced in accordance with the discovery approach, starting from the 2-hydroxyethoxy derivative 14 through the tosyloxy derivative 15 with morpholine in a one-pot reaction. In this way, the indolin-2-one 2 was synthesized from 8 in six steps. Finally, acylation of the indolin-2-one 2 was achieved with the sulfonyl chloride 1 in the presence of KOtBu in dimethyl sulfoxide (DMSO) at room temperature. This synthetic route proved to be applicable for the large-scale synthesis of SR-121463.
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9

Kumar, Praveen, Jai Prakash Kumar, Juhi Barnwal, and Ritu Singh. "Design, Synthesis and Molecular Docking Studies of 4-{3-[2-(2-Morpholin-4-yl-ethoxy)phenyl]-5-phenyl-pyrazol-1-yl}-benzenesulfonamide as Anti-Breast Cancer Agent." Asian Journal of Organic & Medicinal Chemistry 5, no. 4 (December 31, 2020): 301–6. http://dx.doi.org/10.14233/ajomc.2020.ajomc-p271.

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Novel 4-{3-[2-(2-morpholin-4-yl-ethoxy)phenyl]-5-phenyl-pyrazol- 1-yl}benzenesulfonamide (7) was synthesized and evaluated for its anti-breast cancer activity. It was prepared by cyclocondensation reaction of morpholine-substituted β-diketone, 1-[2-(2-morpholin-4-yl-ethoxy)- phenyl]-3-phenyl-propane-1,3-dione (3) with 4-hydrazinobenzenesulfonamide hydrochloride (6). Chemical structure of titled compound (7) was confirmed by FTIR, 1H & 13C NMR and HRMS spectroscoic analyses. The anticancer activity of titled compound 7 was evaluated against MCF-7 breast cancer cell line by MTT assay. Molecular docking was performed to predict its plausible binding with the estrogen receptor α(ERα) using Molecular Operating Environment 2019.0101 software. The MTT assay results showed that titled compound 7 exhibited better anticancer activity against MCF7 cells (IC50: 4.25 μM) than standard drug, 4-hydroxytamoxifen (IC50: 8.22 μM). Results of molecular docking studies were found in good agreement with the results of anticancer evaluation, as the binding score of titled compound 7 (-16.9872 kcal/mol) was lower as compared to 4-hydroxytamoxifen (-15.1112 kcal/mol). The new cationic interaction of titled compound 7 with Trp383 and hydrogen bonding interaction with Phe404 in active site of ERα made its anticancer activity better than 4-hydroxytamoxifen. Thus, 4-{3-[2-(2-morpholin-4-yl-ethoxy)phenyl]-5-phenyl-pyrazol- 1-yl}benzenesulfonamide (7) was emerged as a potent anti-breast cancer agent.
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10

Barker, David, Benjamin Dickson, Nora Dittrich, and Claire E. Rye. "An acyl-Claisen approach to the synthesis of lignans and substituted pyrroles." Pure and Applied Chemistry 84, no. 7 (March 25, 2012): 1557–65. http://dx.doi.org/10.1351/pac-con-11-09-27.

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The acyl-Claisen rearrangement, also called a zwitterionic aza-Claisen rearrangement, allows for the synthesis of 2,3-syn-substituted morpholine pent-4-eneamides with high levels of diastereoselectivity. A wide variety of alkyl and aryl substituents can be introduced with yields highly dependent on the stoichiometry of the Lewis acid catalyst. The use of these morpholine amides in the synthesis of the tetrasubstituted tetrahydrofuran lignans fragransin A2, talaumidin, and galbelgin is summarized. The conversion of the Claisen-derived amides into aryl tetraline and 1,1-diarylbutanol lignans via alteration of the protecting groups is also described. Nucleophilic addition of an organometallic reagent to the morpholine amide followed by Wacker oxidation of the alkene gives highly substituted 1,4-diketones, which can be easily converted into fully substituted pyrroles.
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11

Wang, Dan, Yifu Wang, Heting Wan, Jilin Wang, and Lulu Wang. "Synthesis of gemini basic ionic liquids and their application in anion exchange membranes." RSC Advances 8, no. 19 (2018): 10185–96. http://dx.doi.org/10.1039/c8ra00594j.

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A gemini-type basic morpholine ionic liquid ([Nbmd][OH]) was synthesizedviaa two-step method with morpholine, bromododecane and 1,4-dibromobutane as raw materials, and its structure was characterized by1H NMR and FT-IR spectroscopy.
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12

Shi, Qian-Ping, Zhi-Hao Shi, Nian-Guang Li, Yu-Ping Tang, Hao Tang, Wei Zhang, Min-Zhe Shen, et al. "Efficient Chemical Synthesis of a Scutellarein Derivative Containing Morpholine Ring." Letters in Organic Chemistry 11, no. 8 (June 2014): 590–95. http://dx.doi.org/10.2174/1570178611666140421230118.

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13

Nikitin, Evgeny, Georgy Shumatbaev, Dmitriy Terenzhev, Kirill Sinyashin, and Egor Rastergaev. "New Sintanyl Phosphonates for Protection of Oil and Gas Pipelines from Steel Corrosion." Civil Engineering Journal 5, no. 4 (April 27, 2019): 789–95. http://dx.doi.org/10.28991/cej-2019-03091288.

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Many corrosion inhibitors are economically disadvantageous or toxic to the environment. Additionally, there are certain requirements for corrosion inhibitors. Therefore, the development of new corrosion inhibitors is one of the important problems in the oil-producing and oil-refining industry. The purpose of this work is the synthesis of new corrosion inhibitors with high inhibitory activity, the establishment of the structure of the compounds obtained and the determination of the anti-corrosion effect with respect to aggressive media. This paper presents the results of research on the development of new iron corrosion inhibitors. New α-aminophosphonates were synthesized based on the Kabachnik-Fields reaction. Formalin, morpholine, phosphite containing residues of industrial non-ionic surfactants - syntanols as radicals were used as a raw material. The compounds obtained were isolated in high yield. The structure of the compounds obtained is established by modern methods of physico-chemical analysis. The protective effect of the compounds obtained was studied by a gravimetric method for 6, 24, 72 hour exposure and an inhibitor concentration of 10, 25, 50, 100 ppm. As an aggressive medium, a highly mineralized medium containing СО2 and Н2S was used in simulated formation water. The dynamics of changes in the protective effect of the resulting aminophosphonate from time to time, at dosages of 2.5-100 ppm, were studied using electrochemical analysis methods. The protective effect of syntanyl-O-ethyl- (N-morpholinyl) methylphosphonate obtained at 25 ppm and a shutter speed of 6 hours is 73-82%. The article shows that with increasing concentration, an increase in the protective effect is observed. The greatest protective (89,6) effect showed O-2- [2- [2- [2- [2- [2- [2- [2- [2- [2- (dodecyloxy) ethoxy] ethoxy] ethoxy] ethoxy ] ethoxy] ethoxy] ethoxy] ethoxy] ethoxy] ethyl-O-ethyl- (N-morpholinyl) methylphosphone at a dosage of 100 ppm.
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14

Liu, Chunjing, Benyi Li, and Lester Mitscher. "Synthesis of New TGX-221 Analogs." Zeitschrift für Naturforschung B 69, no. 7 (July 1, 2014): 817–22. http://dx.doi.org/10.5560/znb.2014-4081.

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TGX-221 is a potent phosphoinositide 3-kinase (PI3K)β inhibitor that has great therapeutic potential to treat prostate cancer. Chemical modification of TGX-221 at positions 2 and 9 was made. Five new TGX-221 analogs with different heterocyclic substituents of morpholine, 1-methylpiperazine, aniline, and thiazole-2-amine at positions 2 and 9 were synthesized. Parallel synthetic methods were employed in SN2 replacement reactions at positions 2 and 9 of TGX-221.
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15

Al-Wasidi, Asma S., Nawal M. Al-Jafshar, Amal M. Al-Anazi, Eid H. Alosaimi, Moamen S. Refat, Lamia El-Zayat, Mohamed A. Al-Omar, Ahmed M. Naglah, and K. M. Abou El-Nour. "Electron-transfer complexation of morpholine donor molecule with some π – acceptors: Synthesis and spectroscopic characterizations." Polish Journal of Chemical Technology 21, no. 4 (December 1, 2019): 82–88. http://dx.doi.org/10.2478/pjct-2019-0043.

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Abstract Morpholine is an interesting moiety that used widely in several organic syntheses. The intermolecular charge-transfer (CT) complexity associated between morpholine (Morp) donor with (monoiodobromide “IBr”, 2,3-dichloro-5,6-dicyano-1,4-benzoquinone “DDQ”, 2,6-dichloroquinone-4-chloroimide “DCQ” and 2,6-dibromoquinone-4-chloroimide “DBQ”) π–acceptors have been spectrophotometrically investigated in CHCl3 and/or MeOH solvents. The structures of the intermolecular charge-transfer (CT) were elucidated by spectroscopic methods like, infrared spectroscopy. Also, different analyses techniques such as UV-Vis and elemental analyses were performed to characterize the four morpholine [(Morp)(IBr)], [(Morp)(DDQ)], [(Morp)(DCQ)] and [(Morp)(DBQ)] CT-complexes which reveals that the stoichiometry of the reactions is 1:1. The modified Benesi-Hildebrand equation was utilized to determine the physical spectroscopic parameters such as association constant (K) and the molar extinction coefficient (ε).
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16

Ahmadi, Abbas, Mohsen Khalili, Ramin Hajikhani, and Moslem Naserbakht. "New morpholine analogues of phencyclidine: Chemical synthesis and pain perception in rats." Pharmacology Biochemistry and Behavior 98, no. 2 (April 2011): 227–33. http://dx.doi.org/10.1016/j.pbb.2010.12.019.

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17

Cámara, Fernando, Linda Pastero, Rossella Arletti, and Monica Cagnoni. "A novel layered aluminophosphate with corner-sharing AlO6chains." Acta Crystallographica Section A Foundations and Advances 70, a1 (August 5, 2014): C993. http://dx.doi.org/10.1107/s2053273314090068.

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The synthesis, Raman spectroscopy and crystal structure of a novel layered aluminophosphate is described. The new phase was derived by the sol-gel method starting from a modified low hydrothermal ALPO4-34 zeolite synthesis procedure[1].The structure was solved by direct methods using single-crystal X-ray diffraction. The synthesized layered material, with composition [AlPO3(OH)F(H2O)]-(H9C4ON), crystallizes in the monoclinic space group P21/a with a = 9.2282(5) Å, b = 6.9152(4) Å, c = 14.4615(9) Å, β = 101.57(1)0. Layered aluminophosphates with AlO6polyhedra have been previously described [2], although in these compounds Al octahedral share edges. The novel compound has corner sharing AlO4F(H2O) chains along [010], where fluorine is at the shared apex, four oxygen atoms are shared with PO4tetrahedra and the fifth oxygen is a H2O group. This kind of aluminophosphate chains is found in nature in tancoite [3]. Chains are linked along [100] through corner sharing with a PO4group of the adjacent chain plus hydrogen bonding of the H2O group. Layers are stacked along c* through hydrogen bonding with a double layer of morpholine (H9C4ON) molecules. The chemical stability field of the novel materialis strongly dependent from the fluorine/aluminum ratio of the starting gel. At lower fluorine concentrations only ALPO4-34 and/or AlPO4(berlinite) are stable depending on the morpholine content. Crystals growth morphology depends on the supersaturation conditions of the starting gel: at low concentrations crystals are well developed hexagonal like plate shaped and are very thin. At higher concentrations they show a more elongated morphology. A treatment with H2CO3leads to a complete morpholine removal, as shown by in situ Raman spectroscopy. Powder X-ray diffraction reveals that after morpholine extraction, the material diffract still coherently in two dimensions while a strong broadening is shown for basal planes.
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18

Yien, Yvette Y., Caiyong Chen, Jiahai Shi, Liangtao Li, Daniel E. Bauer, Nicholas Huston, Paul D. Kingsley, et al. "Fam210b Is Required for Optimal Cellular and Mitochondrial Iron Uptake during Erythroid Differentiation." Blood 126, no. 23 (December 3, 2015): 405. http://dx.doi.org/10.1182/blood.v126.23.405.405.

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Abstract Red cells synthesize large quantities of heme during terminal differentiation. Central to erythropoiesis is the transport and trafficking of iron within the cell. Despite the importance of iron transport during erythroid heme synthesis, the molecules involved in intracellular trafficking of iron are largely unknown. In a screen for genes that are up-regulated during erythroid terminal differentiation, we identified FAM210B, a predicted multi-pass transmembrane mitochondrial protein as an essential component of mitochondrial iron transport during erythroid differentiation. In zebrafish and mice, Fam210b mRNA is enriched in differentiating erythroid cells and liver (fetal and adult), which are tissues that require large amounts of iron for heme synthesis. Here, we report that FAM210B facilitates mitochondrial iron import during erythroid differentiation and is essential for hemoglobin synthesis. Zebrafish are anemic when fam210b is silenced using anti-sense morpholinos (Fig. A). CRISPR knockout of Fam210b caused a heme synthesis defect in differentiating Friend murine erythroleukemia (MEL) cells. PPIX levels in Fam210b deficient cells are normal, demonstrating that Fam210b does not participate in synthesis of the heme tetrapyrrole ring. Consistent with this result, supplementation of Fam210b deficient MEL cells with either aminolevulinic acid, the first committed substrate of the heme synthesis pathway or a chemical analog of protoporphyrin IX failed to chemically complement the heme synthesis defect. While Fam210b was not required for basal housekeeping heme synthesis, Fam210b deficientcells showed defective total cellular and mitochondrial iron uptake during erythroid differentiation (Fig. B). As a result, Fam210b deficient cells had defective hemoglobinization. Supplementation of Fam210b-/- MEL cells with non-transferrin iron chelates restored erythroid differentiation and hemoglobin synthesis; whereas, similar chemical complementation could not be achieved in the Tmem14c-/- cells, which have a primary defect in tetrapyrrole transport. (Fig. C). Our findings reveal that FAM210B is required for optimal mitochondrial iron import during erythroid differentiation for hemoglobin synthesis. It may therefore function as a genetic modifier for mitochondriopathies, anemias or porphyrias. Figure 1. Figure 1. Disclosures Bauer: Biogen: Research Funding; Editas Medicine: Consultancy. Orkin:Editas Inc.: Consultancy.
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19

Kravchenko, Dmitri V., Volodymyr M. Kysil, Alexey P. Ilyn, Sergey E. Tkachenko, Sergey Maliarchouk, Ilya M. Okun, and Alexandre V. Ivachtchenko. "Synthesis and Chemical Transformations of 6‐(Morpholine‐4‐sulfonyl)‐quinoline‐2,3,4‐tricarboxylic Acid." Synthetic Communications 36, no. 7 (March 1, 2006): 911–17. http://dx.doi.org/10.1080/00397910500466165.

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20

Trabocchi, Andrea, Duccio Cavalieri, and Antonio Guarna. "Chemical genetics approach to drug discovery by diversity-oriented synthesis (DOS) of peptidomimetics." Pure and Applied Chemistry 83, no. 3 (January 18, 2011): 687–98. http://dx.doi.org/10.1351/pac-con-10-09-30.

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Chemical genetics, which relies on selecting small molecules for their ability to induce a biological phenotype or to interact with a particular gene product, is a new powerful tool for lead generation in drug discovery. Accordingly, diversity-oriented synthesis (DOS) of small-molecule peptidomimetics gives access to collections of new chemotypes bearing high structural diversity. Biological evaluation using cell growth as a phenotypic screening on Saccharomyces cerevisiae deletant strains is a powerful tool to identify new chemotypes as hit compounds in the discovery of new antifungal and anticancer agents, and also in the dissection of their mode of action. Our contribution in this field focused on the screening of morpholine-based peptidomimetic collections toward yeast deletant strains, which provided the identification of new chemotypes involved in mitochondria metabolism and respiration.
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21

Kanagarajan, V., J. Thanusu, and M. Gopalakrishnan. "A Green Chemical Approach towards the 'One-Pot' Synthesis, Spectral Characterization and in Vitro Antibacterial and Antifungal Activities of Morpholino Pyrimidines." Journal of the Korean Chemical Society 53, no. 6 (December 20, 2009): 731–41. http://dx.doi.org/10.5012/jkcs.2009.53.6.731.

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22

Kanagarajan, Vijayakumar, Jayaraman Thanusu, and Mannathusamy Gopalakrishnan. "Design, Synthesis and Spectral Characterization of Novel 2-morpholino-N-(4,6-diarylpyrimidin-2-yl)acetamides." Journal of the Korean Chemical Society 54, no. 1 (February 20, 2010): 49–54. http://dx.doi.org/10.5012/jkcs.2010.54.01.049.

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23

Fonseca, Renilma S. P., Fernando C. Silva, Francisco S. M. Sinfrônio, Caritas de J. S. Mendonça, and Inocêncio S. dos S. Neto. "SYNTHESIS OF MORPHOLINE-BASED IONIC LIQUIDS FOR EXTRACTIVE DESULFURIZATION OF DIESEL FUEL." Brazilian Journal of Chemical Engineering 36, no. 2 (June 2019): 1019–27. http://dx.doi.org/10.1590/0104-6632.20190362s20180107.

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24

Sperlich, Jörg, Joachim Becht, Mathias Mühleisen, Stephan A. Wagner, Günter Mattern, and Reinhold Tacke. "Zwitterionische Bis[vic-arendiolato(2 –)] [(morpholinio)alkyl]silicate: Synthese sowie strukturelle Charakterisierung in Lösung und im Kristall / Zwitterionic Bis[vic-arenediolato(2 –)] [(morpholinio)alkyl]silicates: Synthesis and Structural Characterization in Solution and in the Crystal." Zeitschrift für Naturforschung B 48, no. 12 (December 1, 1993): 1693–706. http://dx.doi.org/10.1515/znb-1993-1201.

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The zwitterionic A5-spirosilicates bis[1,2-benzenediolato(2–)][(morpholinio)methyl]silicate (1), bis[2,3-naphthalenediolato(2–)][(morpholinio)methyl]silicate (2; isolated as 2 • CH3CN), bis[1,2-benzenediolato(2–)][3-(morpholinio)propyl]silicate (3) and bis[2,3-naphthalenediolato(2 –)][3-(morpholinio)propyl]silicate (4; isolated as 4·1/2CH3CN) have been synthesized by various methods including Si – C bond cleavage reactions. The crystal structures of 2 • CH3CN and 4 · 1/2 CH3CN have been determined. 1,2 • CH3CN, 3 and 4 · 1/2 CH3CN have also been characterized by solution-state (1H, 13C, 29Si) and solid-state NMR spectroscopy (29Si CP/MAS). The pentacoordinate silicon atoms of the zwitterions 1-4 are surrounded by four oxygen atoms and one carbon atom. In the crystal, the coordination polyhedra around the silicon atoms of 2 • CH3CN (two crystallographically independent zwitterions and two crystallographically independent acetonitrile molecules) can be described as nearly ideal trigonal bipyramids, with the carbon atoms occupying equatorial sites. The crystal structure of 2 • CH3CN is considerably influenced by intermolecular N – H···N hydrogen bonds between the zwitterions and the acetonitrile molecules. The coordination polyhedron observed for the silicon atom in the crystal of 4 · 1/2 CH3CN can be described as a distorted square pyramid, with the carbon atom in the apical position. The crystal structure of 4 · 1/2 CH3CN is considerably governed by intermolecular N –H···O hydrogen bonds between the zwitterions which form infinite chains in the crystal. The 29Si chemical shifts (δ = – 75,5 to – 85,8) observed for 1,2 • CH3CN, 3 and 4 · 1/2 CH3CN in solution ([D6]DMSO) and in the crystal are typical of pentacoordinate silicon of the type SiO4C. For all compounds very similar 29Si chemical shifts have been observed for the solution and solid state [⊿(δ29Si) ≤ 0,9] indicating that the zwitterions 1-4 do also exist in solution.
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Tiwari, Shailee V., Julio A. Seijas, M. Pilar Vazquez-Tato, and Anna Pratima G. Nikalje. "Ultrasound Assisted Synthesis of Diethyl (2-(1-(morpholinomethyl)-2-Oxoindolin-3-ylidene)hydrazinyl) (Substituted Phenyl/heteryl) MethylphosphonateDerivatives." Proceedings 9, no. 1 (November 14, 2018): 3. http://dx.doi.org/10.3390/ecsoc-22-05790.

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This work reports ultrasound assisted synthesis diethyl (2-(1-(morpholinomethyl)-2-oxoindolin-3-ylidene)hydrazinyl) (substituted phenyl/heteryl) methylphosphonate 9(a–j) derivatives. The derivatives are synthesized using a green protocol. In the first step, 3-hydrazonoindolin-2-one is synthesized using ultrasound. In the second step, diethyl (substituted phenyl/heteryl)(2-(2-oxoindolin-3-ylidene)hydrazinyl) methylphosphonate 6(a–j) derivatives are synthesized using cerric ammonium nitrate as catalyst. In the third step, diethyl (2-(1-(morpholinomethyl)-2-oxoindolin-3-ylidene)hydrazinyl) (substituted phenyl/heteryl) methylphosphonate 9(a–j) derivatives are synthesized using ultrasound. Isatin, chemically known as H-indole-2,3-dione, and its derivatives possess a broad range of biological and pharmacological properties. Isatin is widely used as a starting material for the synthesis of a broad range of heterocyclic compounds and as substrates for drug synthesis. The α-amino phosphonate derivatives constitute an important class of organophosphorus compounds on account of their versatile biological activity. Morpholine moiety has been found to be an eminent pharmacophore in medicinal chemistry. A number of molecules possessing morpholine moiety are clinically approved drugs. The importance of this ring is well understood by medicinal chemists, since they play a major role in molecular properties such as an electronic distribution, three dimensionality, scaffold flexibility/rigidity, lipophilicity or polarity and metabolic stability. Considering the importance of the three pharmacophores, this promoted us to club these pharmacophores together in a single molecule using a green synthetic protocol.The structures of the ultrasound synthesized compounds were confirmed by spectral analysis like IR, 1H NMR, 13C NMR, 31P NMR and MS.
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26

Buron, Frédéric, Nuno Rodrigues, Thibault Saurat, Marie Aude Hiebel, Stéphane Bourg, Pascal Bonnet, Reine Nehmé, et al. "Design, Synthesis and SAR in 2,4,7-Trisubstituted Pyrido[3,2-d]Pyrimidine Series as Novel PI3K/mTOR Inhibitors." Molecules 26, no. 17 (September 2, 2021): 5349. http://dx.doi.org/10.3390/molecules26175349.

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This work describes the synthesis, enzymatic activities on PI3K and mTOR, in silico docking and cellular activities of various uncommon 2,4,7 trisubstituted pyrido[3,2-d]pyrimidines. The series synthesized offers a chemical diversity in C-7 whereas C-2 (3-hydroxyphenyl) and C-4 groups (morpholine) remain unchanged, in order to provide a better understanding of the molecular determinants of PI3K selectivity or dual activity on PI3K and mTOR. Some C-7 substituents were shown to improve the efficiency on kinases compared to the 2,4-di-substituted pyrimidopyrimidine derivatives used as references. Six novel derivatives possess IC50 values on PI3Kα between 3 and 10 nM. The compounds with the best efficiencies on PI3K and mTOR induced micromolar cytotoxicity on cancer cell lines possessing an overactivated PI3K pathway.
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27

Sánchez García, Jessica J., Marcos Flores-Alamo, Mark E. Martínez Klimov, and Elena I. Klimova. "N-alkyl-2-(1,2-diferrocenylvinyl)-4,5-dihydrooxazolinium salts, multi-component synthesis and breaking of their heterocyclic systems." Pure and Applied Chemistry 88, no. 12 (December 1, 2016): 1129–42. http://dx.doi.org/10.1515/pac-2016-0812.

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AbstractA new multicomponent method for the synthesis of N-alkyl-2-(Z-1,2-diferrocenylvinyl)-4,5-dihydrooxazolinium salts 3a–f, 5-(N-alkyl-2′,3′-diferrocenyl-acryloylamido)-3-aza-3-alkylpentanols 4a–d, (E)-N-alkyl-N-(2-morpholinoethyl)-2,3-diferrocenylacrylamides 9a,b,e,f and (E)-N-alkyl-N-(2-piperidinoethyl)-2,3-diferrocenylacrylamides 10a,c from reactions of 2,3-diferrocenylcyclopropenone 1 with bis-1,4-N,O-nucleophiles in the presence of triethyloxonium tetrafluoroborate, alkyl iodides, morpholine, piperidine and Et3N is described. The characterization of the new compounds was done by IR, 1H- and 13C-NMR spectroscopy, mass-spectrometry, elemental analysis and X-ray diffraction studies.
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28

Grbović, Ljubica, Bojana Radovan Vasiljević, Ksenija Pavlović, Timea Hajnal-Jafari, Simonida Đurić, Mirjana Popsavin, and Slavko Kevrešan. "Microwave-assisted synthesis of biologically active amide derivatives of naphthenic acids under neat conditions." Macedonian Journal of Chemistry and Chemical Engineering 37, no. 1 (June 9, 2018): 13. http://dx.doi.org/10.20450/mjcce.2018.1371.

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Within the field of green chemistry, a noticeable results were obtained in the solvent-free synthesis of amide derivatives of naphthenic acids under microwave irradiation. Naphthenic acid amides, anilides, and morpholides were synthesized directly from free carboxylic acids and amines in the absence of solvent and catalyst under high-temperature heating in a closed-vessel system of microwave reactor. With this new and efficient method, different primary, secondary, and tertiary amide derivatives of naphthenic acids were obtained in good to excellent yields. Synthesized derivatives were assayed as plant rooting agents for their stimulative effects on the formation of adventitious roots in sunflower cuttings and susceptibility for growth stimulation of Pseudomonas sp. strains.
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29

Kanagarajan, V., and M. Gopalakrishnan. "Morpholino pyrimidinyl acetamides: design, green chemical one-pot synthesis, and in vitro microbiological evaluation." Pharmaceutical Chemistry Journal 45, no. 3 (June 2011): 170–77. http://dx.doi.org/10.1007/s11094-011-0586-y.

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30

Patel, K. C., S. N. Kaula, and P. S. Patel. "Synthesis and Physico-Chemical Properties of 2-Morpholino-4,6-Dichloro-S-Triazine with Various Aromatic Diols." High Performance Polymers 8, no. 2 (June 1996): 265–73. http://dx.doi.org/10.1088/0954-0083/8/2/007.

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Several homopolycyanurates were synthesized by stirred interfacial polycondensation of 2-morpholino-4,6-dichloro- s-triazine with various aromatic diols such as 1,5- dihydroxynaphthalene,(DHN-1,5),1,7-dihydroxynapthalene(DHN-1,7),2,7-dihydroxynapthalene resorcinol (R), catechol (C), hydroquinone (H) and phenolphthalein (Ph). They were characterized by density, viscosity measurements, IR spectra, solubility tests and thermogravimetric analysis. The polymer had reduced viscosities in the range 0.468 to 0.829 dl g−1 in chromoform at 30 °C. All the polymers were amorphous and soluble in chlorinated solvents. The thermal stability of polycyanurates decreases in the following matter: PCDHN-1,5 > PCDHN-1,7 > PCPh > PCR ≃ PCDHN-2,7 > PCHQ > PCC.
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31

Hassanain, Hawazen, E. Stephen Davies, William Lewis, Deborah L. Kays, and Neil R. Champness. "Morpholino-Substituted BODIPY Species: Synthesis, Structure and Electrochemical Studies." Crystals 10, no. 1 (January 14, 2020): 36. http://dx.doi.org/10.3390/cryst10010036.

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Functionalization of 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene (BODIPY) chromophores at the 2,6-positions with iodo substituents and morpholino-substituted α-methyl groups affords molecules with strong absorbance in the visible spectrum. The effect of such substitution on the solid-state arrangements, absorption, fluorescence and electronic properties of these dye molecules is reported. The spectroscopic and spectroelectrochemical measurements display intense absorptions in the UV-visible spectrum with bathochromic shifts, in comparison to unfunctionalized BODIPY, and a positive shift in redox potentials due to functionalisation of the BODIPY core. Halogen bonds are observed in the solid-state structures of both halogenated BODIPY species, which in one case leads to the formation of an unusual halogen bonded framework.
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32

Parra, Marilyn, Xiuli An, Narla Mohandas, and John G. Conboy. "In Vivo Analysis of Erythroid Protein 4.1 Pre-mRNA Splicing Mechanisms: Use of Antisense Morpholinos to Assay Function of Deep Intron Regulatory Elements." Blood 116, no. 21 (November 19, 2010): 815. http://dx.doi.org/10.1182/blood.v116.21.815.815.

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Abstract Abstract 815 Erythroid stage-specific alternative splicing plays an essential role in the expression of protein 4.1R isoforms that interact with other skeletal proteins to strengthen the membrane. In late erythroblasts, 4.1R mRNA is processed from pre-mRNA that initiates transcription at alternative first exon 1A (E1A) and splices exclusively to the more distal of two alternative 3' splice sites at exon 2 (E2dis), ~100kb downstream. This splicing event is important because it is required to generate the shorter N-terminal domain characteristic of 80kDa isoforms of 4.1R protein in red cells. We have reported that E1A splicing to E2dis requires two nested intrasplicing events mediated by an essential deep intron element originally annotated as exon 1B. However, these studies employed small minigenes transfected into cultured cells, an artificial system that may not correctly reflect in vivo mechanisms. Here we used an antisense RNA strategy to explore splicing of endogenous full length 4.1R pre-mRNA in tissues of live mice and in primary erythroblasts. Chemically modified oligonucleotides known as vivo-morpholinos (vMOs), introduced via tail vein injection and internalized into selected organs, can base pair with complementary cellular RNA sequences and block function of candidate regulatory motifs. Importantly, two independent vMOs directed against the 4.1R intraexon regulatory element both substantially abrogated intrasplicing in several mouse tissues, robustly switching E1A splicing from E2dis to the proximal 3' splice site in E2 (E2prox). This switch results in inclusion of start codon AUG1 in mature 4.1R mRNA and synthesis of larger isoforms of 4.1R protein. These results were highly sequence-specific, since negative control vMOs directed against other genes did not alter E1A splicing to E2dis. Interestingly, we have recently used vMOs to confirm the existence of a similar deep intron element required for analogous E1A-E2dis splicing in the paralogous 4.1B gene. Together these findings strongly support the in vivo physiological function of deep intron elements in the control of intrasplicing in both 4.1R and 4.1B pre-mRNAs. To test whether the 4.1R intrasplicing mechanism is also active in erythroid cells, we incubated mouse splenic erythroblasts isolated from FVA-treated animals with morpholinos directed against the intraexon. Two independent morpholinos against its 5' splice site and branch point both induced a concentration-dependent switch in E1A splicing from E2dis to E2prox. Control morpholinos had no effect on E1A splicing. Because the splicing switch results in inclusion of alternative translation initiation codon AUG1, it was predicted to induce synthesis of larger isoforms of 4.1R including the N-terminal headpiece known to influence 4.1R binding affinities for other skeletal proteins. Western blot analysis of erythroblast proteins confirmed a switch to expression of larger 4.1R protein isoforms that are not present in normal late stage erythroblasts. Intrasplicing is mediated by deep intron elements, and is essential for accurate physiological splicing of natural 4.1R pre-mRNA in erythroid and other cells. Antisense morpholinos represent a new tool for alternative splicing studies in vivo or in cultured erythroblasts. Disclosures: No relevant conflicts of interest to declare.
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33

El-Samahy, Fatma A., Hayam A. Abd El Salam, Naglaa F. El-Sayed, Elsayed M. Shalaby, and Mahmoud F. Dondeti. "Synthesis of unexpected novel bis-coumarin derivatives via three component reactions of 4-hydroxycoumarin, aldehydes and cyclic secondary amines. Conformation in the solid state and pharmacological evaluation." Zeitschrift für Naturforschung B 72, no. 10 (September 26, 2017): 705–16. http://dx.doi.org/10.1515/znb-2017-0066.

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AbstractA series of unexpected bis-coumarins have been synthesized by multicomponent reactions of 4-hydroxycoumarin, aldehydes, and cyclic secondary amines in ethanol at room temperature. The chemical structures of new compounds were identified by 1H, 13C NMR, and mass spectrometry. Furthermore, the molecular structure of the solid-state adduct of 3,3′-[(4-methoxyphenyl)-methylene]bis(4-hydroxy-2H-chromen-2-one) with morpholine (1:1) has been confirmed by single-crystal X-ray diffraction. The cytotoxicity of the new coumarin derivatives against MCF7 breast cancer cells was evaluated. A docking study of the new products was carried out to assess the molecular affinity between the tested compound and Topoisomerase IIa.
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34

García, L., J. Palazón, J. Gálvez, and G. López. "Synthesis and thermal behaviour of morpholine complexes with cobalt (II) and manganese (II) thiocyanates." Journal of Thermal Analysis 35, no. 1 (January 1989): 113–20. http://dx.doi.org/10.1007/bf01914270.

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35

Enchev, D. D. "Synthesis and Chemical Behavior of the N-Morpholino- O-Alkyl-3-Methyl-1,2-Butadienephosphonic Acid Esters." Phosphorus, Sulfur, and Silicon and the Related Elements 180, no. 9 (September 1, 2005): 2131–35. http://dx.doi.org/10.1080/104265090917637.

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36

Enchev, D. D. "SYNTHESIS AND CHEMICAL BEHAVIOR OF THE N-MORPHOLINO-O-ALKYL-3-METHYL- 1,2-BUTADIENEPHOSPHONIC ACID ESTERS." Phosphorus, Sulfur, and Silicon and the Related Elements 134, no. 1 (March 1, 1998): 431–36. http://dx.doi.org/10.1080/10426509808043620.

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37

Enchev, D. D. "Synthesis and Chemical Behavior of the N-Morpholino-O-Alkyl-3-Methyl-1,2-Butadienephosphonic Acid Esters." Phosphorus, Sulfur, and Silicon and the Related Elements 134, no. 1 (February 1, 1998): 431–36. http://dx.doi.org/10.1080/10426509808545484.

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38

Biçak, Niyazi, A. Bahattin Soydan, and Sedat Çakaloğlu. "Synthesis of N-allyl morpholine and its copolymers with sulfur dioxide and styrene." Designed Monomers and Polymers 1, no. 3 (January 1998): 305–13. http://dx.doi.org/10.1163/156855598x00035.

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39

Djigoue, Guy Bertrand, and Donald Poirier. "Introducing Molecular Diversity at the C20-position of Pregnenolone by the Formation of Spiro-2-morpholinones." Current Organic Synthesis 15, no. 4 (June 12, 2018): 541–51. http://dx.doi.org/10.2174/1570179414666171107161304.

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Aim and Objective: The development of small molecules that can interact with key therapeutic target represents an active field of research. Therefore, new approaches for increasing the molecular diversity of a starting material, such as a natural product, are needed. Herein, the carbonyl group present on a pregnane scaffold, or easily obtained from the oxidation of the corresponding alcohol, was used to obtain a series of diversified steroidal morpholinone derivatives. Materials and Methods: Using chemical synthesis, two levels of molecular diversity were introduced at position 20 of a C21-steroid scaffold. Nuclear magnetic resonance (NMR) spectroscopy and x-ray analysis were next used to characterize the morpholinone derivatives. Results: The C-20 carbonyl of pregnenolone was first transformed into an oxirane that reacted with an amino acid and the resulting amino alcohol was then cyclized to generate different spiro-2-morpholinones. X-ray analysis of one representative compound confirmed the 3-dimensional representation of this new family of diversified steroid derivatives. NMR analysis supported the expected structure and identified key markers of the chiral center configuration found in the 2-morpholinone moiety. Finally, the NH of the morpholinone ring was alkylated, thus increasing structural diversity. Conclusion: Considering the huge amount of building blocks (amino acids, bromobenzyl derivatives and ketones) that are commercially available, the strategy reported herein opens the door to the synthesis of diversified libraries of new compounds.
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40

Khanra, Tapan Kumar, Basudam Adhikari, and Sukumar Maiti. "Multifunctional Activities of Benzazole Derivatives in Rubber Vulcanization." Rubber Chemistry and Technology 66, no. 1 (March 1, 1993): 30–37. http://dx.doi.org/10.5254/1.3538297.

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Abstract Benzazole thiol (e.g. 2-Mercaptobenzothiazole and 2-Mercaptobenzimidazole) and sulfenamide (e.g. 2-Morpholino thiobenzothiazole) are used as rubber chemicals. The nature and the extent of their performances in rubber depend on the nature of the key heteroatom present in the azole ring. It has been found that the presence of X (S or N) as the key heteroatom in the grouping —X—‖—SH of the azole ring is responsible for either accelerator or antioxidant action. Although some scattered informations on accelerator and antioxidant functions are available for some of the benzazole derivatives, their comparative ratings in these functions are not found in the literature. In the present communication, synthesis and characterization of some benzazole sulfenamides are reported. Together with this, a comparative evaluation of accelerator-cum-anti-oxidant properties of both the benzazole thiols and sulfenamides is described. Such dual function rubber chemicals are unusual and novel and should fetch a premium price as rubber additives.
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41

Meenarathi, B., P. Siva, M. Jeyapriya, R. Baskaran, and R. Anbarasan. "Synthesis, Characterization, Catalytic Reduction, and Splinting Activity of Poly(ε-caprolactone-co -morpholine)/Ag Nanocomposite." Advances in Polymer Technology 37, no. 2 (February 12, 2016): 390–98. http://dx.doi.org/10.1002/adv.21678.

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42

Soliman, Saied M., Hessa H. Al-Rasheed, and Ayman El-Faham. "Synthesis, X-ray Structure, Hirshfeld Analysis of Biologically Active Mn(II) Pincer Complexes Based on s-Triazine Ligands." Crystals 10, no. 10 (October 13, 2020): 931. http://dx.doi.org/10.3390/cryst10100931.

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Herein, the synthesis and antimicrobial activities of [Mn(MorphBPT)(H2O)2NO3]NO3; (1) and [Mn(PipBPT)(H2O)2NO3]NO3; (2) complexes of the pincer-type tridentate ligands MorphBPT; 4-(4,6-di(1H-pyrazol-1-yl)-1,3,5-triazin-2-yl)morpholine and PipBPT; 2-(piperidin-1-yl)-4,6-di(1H-pyrazol-1-yl)-1,3,5-triazine are presented. Both complexes have slightly distorted octahedral coordination geometry. Their molecular packing depends on O–H···O, C–H···O hydrogen bonds and anion–π stacking contacts. Hirshfeld analysis was used to quantify the different contacts. Both complexes exhibited better anti-fungal activity than the standard Fluconazole and comparable antibacterial activity to Gentamycin against Staphylococcus aureus and Escherichia coli microbes. Moreover, complexes 1 and 2 are biologically more active than the free ligands against these microbes.
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43

Abu-Hashem, Ameen Ali, Sami A. Al-Hussain, and Magdi E. A. Zaki. "Synthesis of Novel Benzodifuranyl; 1,3,5-Triazines; 1,3,5-Oxadiazepines; and Thiazolopyrimidines Derived from Visnaginone and Khellinone as Anti-Inflammatory and Analgesic Agents." Molecules 25, no. 1 (January 5, 2020): 220. http://dx.doi.org/10.3390/molecules25010220.

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Novel (4-methoxy or 4,8-dimethoxy)-3-methyl-N-(6-oxo-2-thioxo-1,2,3, 6-tetrahydro- pyrimidin-4-yl) benzo [1,2-b: 5, 4-b’] difuran-2-carboxamide (5a–b) has been synthesized by the reaction of visnagenone–ethylacetate (2a) or khellinone–ethylacetate (2b) with 6-aminothiouracil in dimethylformamide or refluxing of benzofuran-oxy-N-(2-thioxopyrimidine) acetamide (4a–b) in sodium ethoxide to give the same products (5a,b) in good yields. Thus, compounds 5a–b are used as an initiative to prepare many new heterocyclic compounds such as 2-(4-(3-methylbenzodifuran- 2-carbox-amido) pyrimidine) acetic acid (6a–b), N-(thiazolo[3, 2-a]pyrimidine)-3-methylbenzo- difuran-2-carboxamide (7a–b), N-(2-thioxopyrimidine)-methylbenzodifuran-2-carbimidoylchloride (8a–b), N-(2-(methyl-thio) pyrimidine)-3-methylbenzodifuran-2-carbimidoylchloride (9a–b), N-(2, 6 -di(piperazine or morpholine)pyrimidine)-1-(3-methylbenzodifuran)-1-(piperazine or morpholine) methanimine(10a–d), 8-(methylbenzodifuran)-thiazolopyrimido[1,6-a][1,3,5]triazine-3,5-dione (11a –b), 8-(3-methyl benzodifuran)-thiazolopyrimido[6,1-d][1,3,5]oxadiazepine-trione (12a–b), and 2,10 -di(sub-benzylidene)-8-(3-methylbenzodifuran)-thiazolopyrimido[6,1-d][1,3,5]oxadiazepine-3,5,11- trione (13a–f). All new chemical structures were illustrated on the basis of elemental and spectral analysis (IR, NMR, and MS). The new compounds were screened as cyclooxygenase-1/ cyclooxygenase-2 (COX-1/COX-2) inhibitors and had analgesic and anti-inflammatory activities. The compounds 10a–d and 13a–f had the highest inhibitory activity on COX-2 selectivity, with indices of 99–90, analgesic activity of 51–42% protection, and anti-inflammatory activity of 68%–59%. The inhibition of edema for the same compounds, 10a–d and 13a–f, was compared with sodium diclofenac as a standard drug.
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44

Khezami, Khaoula, Kevser Harmandar, Esra Bağda, Efkan Bağda, Gamze Şahin, Nurşen Karakodak, Bassem Jamoussi, and Mahmut Durmuş. "The new water soluble zinc(II) phthalocyanines substituted with morpholine groups- synthesis and optical properties." Journal of Photochemistry and Photobiology A: Chemistry 401 (October 2020): 112736. http://dx.doi.org/10.1016/j.jphotochem.2020.112736.

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45

Agarwal, R., M. H. Ansari, M. W. Y. Khan, M. Ahmad, and K. D. Sharma. "Synthesis and antimicrobial activity of fatty 2-morpholinones prepared from epoxy fatty acid methyl esters." Journal of the American Oil Chemists' Society 66, no. 6 (June 1989): 825–27. http://dx.doi.org/10.1007/bf02653677.

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46

Palazón, J., J. Gálvez, G. García, and G. López. "Synthesis and thermal study of some adducts of morpholine with nickel(II) nitrite, sulphate and perchlorate." Journal of Thermal Analysis 32, no. 2 (March 1987): 645–52. http://dx.doi.org/10.1007/bf01912717.

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47

Ma, Da-You, Li-Chao Zhang, Kun-Jian Peng, Jiang Zeng, Li-Jun Liu, Zhi-Yong Luo, and Su-You Liu. "7-O-aminoalkyl-2,3-dehydrosilibinins: Synthesis and in vitro Anti-cancer Efficacy." Anti-Cancer Agents in Medicinal Chemistry 18, no. 8 (December 28, 2018): 1156–62. http://dx.doi.org/10.2174/1871520618666180402122713.

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Background: The heptaprotective flavonolignan silibinin and dehydrosilibinin have exhibited moderate antiproliferative activities toward many cancer cell lines. Considering of the nontoxic profile of these natural products, chemical modification to enhance the anticancer potentials is promising. Method: A series of 7-O-aminoalkyl-2,3-dehydrosilibinin derivatives were synthesized and evaluated for their antiproliferative activities against several cancer cell lines. Results: A number of the synthesized dehydrosilibinin derivatives exhibited greatly enhanced potency with 50% growth inhibition at low micromolar concentrations. Structure activity study indicated that the distance between N and 7-O on the side chain has a limited influence on the antiproliferative activity, while the presence of a morpholino group decreases the antiproliferative activities dramatically. Flow cytometry based assays on human colon cancer HCT116 cells revealed that 6a and 6c, two of the most potent derivatives, effectively arrested the cell cycle in the G2 phase and stimulated cell apoptosis. Conclusion: Our findings suggest that attaching an appropriate tertiary amino alkyl side chain through 7-Oalkylation on 2,3-dehydrosilibinin, would be a viable strategy for the development of silibinin derivatives as anticancer agents.
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48

Barakat, Assem, Saied M. Soliman, Matti Haukka, Abdullah Mohammed Al-Majid, Mohammad Shahidul Islam, M. Ali, and Mohammed Rafi Shaik. "One-Pot Synthesis, X-ray Single Crystal and Molecular Insight of Enaminone-Based β-Morpholino-/N-Methylpiperazinyl-/Pyrrolidinylpropiophenone." Crystals 10, no. 4 (April 8, 2020): 282. http://dx.doi.org/10.3390/cryst10040282.

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One-pot synthesis of three enaminones, (E)-1-(4-chlorophenyl)-3-morpholinoprop-2-en-1-one 1, (E)-1-(4-chlorophenyl)-3-(4-methylpiperazin-1-yl)prop-2-en-1-one 2, and (E)-1-(4-chlorophenyl)-3-(pyrrolidin-1-yl)prop-2-en-1-one 3 were achieved. The synthetic protocol via three components reaction of p-chloroacetophenone with DMFDMA (N,N-dimethylformamid-dimethylacetal) and the corresponding secondary amines (morpholine/N-methylpiperazine/pyrrolidine) in dioxane under heating for 2.5–4 h at 102 °C yielded the requisite enaminones. This protocol has the advantage of no separation of intermediate, no need for column purification with quantitative yield for the target compounds. The chemical features of the β-enaminones 1–3 were assigned by NMR. β-Enaminones 1, and 2 were assigned by single crystal X-ray diffraction technique. The intermolecular interactions in the crystal structures were analyzed quantitatively using Hirshfeld analysis. The Cl…H and O…H hydrogen bonds are common in both compounds while the C-H…π and N…H contacts are more significant in 2 than 1. DFT studies were investigated to show the electronic and spectroscopic properties (NMR and UV-Vis) of the studied systems.
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49

Zhou, Chuanzheng, Wimal Pathmasiri, Dmytro Honcharenko, Subhrangsu Chatterjee, Jharna Barman, and Jyoti Chattopadhyaya. "High-quality oligo-RNA synthesis using the new 2′-O-TEM protecting group by selectively quenching the addition of p-tolyl vinyl sulphone to exocyclic amino functions." Canadian Journal of Chemistry 85, no. 4 (April 1, 2007): 293–301. http://dx.doi.org/10.1139/v07-025.

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During the F–-promoted deprotection of the oligo–RNA, synthesized using our 2′-O-(4-tolylsulfonyl)ethoxymethyl (2′-O-TEM) group [Org. Biomol. Chem. 5, 333 (2007)], p-tolyl vinyl sulphone (TVS) is formed as a by-product. The TVS formed has been shown to react with the exocyclic amino functions of adenosine (A), guanosine (G), and cytidine (C) of the fully deprotected oligo–RNA to give undesirable adducts, which are then purified by HPLC and unambiguously characterized by 1H, 13C Heteronuclear Multiple Bond Correlation (HMBC) NMR and mass spectroscopic analysis. The relative nucleophilic reactivities of the nucleobases toward TVS have been found to be the following: N6–A > N4–C > N2–G > > N3–U. This reactivity of TVS toward RNA nucleobases to give various Michael adducts could, however, be suppressed by using various amines as scavengers. Among all these amines, morpholine and piperidine are the most efficient scavenger for TVS, which gave highly pure oligo–RNA even in the crude form and can be used directly in RNA chemical biology studies.Key words: RNA synthesis, RNA alkylation, p-tolyl vinyl sulphone, Michael addition.
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50

Suhak, O. A., О. I. Panasenko, and Ye G. Knysh. "Synthesis, physic and chemical properties of 2-(4-R-5-(thiophene-2-ylmethyl)-4h-1,2,4-triazole-3-ylthio)acetate acids and their salts." Farmatsevtychnyi zhurnal, no. 2 (August 14, 2018): 48–54. http://dx.doi.org/10.32352/0367-3057.2.17.06.

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Abstract:
Derivatives of 1,2,4-triazole are inherent in various types of biological activity. They can be used as pesticide and medicinal drugs (anticonvulsants, analgetics, antitumor and antibacterial). In this regard the search of new methods of synthesis and investigation of biological activity of 2-(4-R-5-(thiophene-2-ylmethyl)-4H-1,2,4-triazole-3-ylthio)acetate acids and their salts is relevant nowadays. With the aim of finding the new biologically active compounds 2-(4-R-5-(thiophene-2-ylmethyl)-4H-1,2,4-triazole-3-ylthio)acetate acids and their salts are synthesized, where R is methyl, ethyl, phenyl. The interaction of 4-R-5-(thiophene-2-ylmethyl)-4H-1,2,4-triazole-3-thions with monochloracetate acid in the medium of i-propyl alcohol in the presence of an equivalent amount of alkali the corresponding 2-(4-R-5-(thiophene-2-ylmethyl)-4H-1,2,4 triazole-3-ylthio)acetate acids are obtained on the basis of which the corresponding salts of morpholine, dimethylamine, monoethanolamine, pteridine, ZnSO4 , CuSO4, NaOH and KOH are obtained and the structure of the received compounds was confirmed on the basis of the data of elemental, IR-, 1H-NMR-spectroscopy. The synthesis of 2-(4-R-5-(thiophene-2-ylmethyl)-4H-1,2,4-triazole-3-ylthio) acetate acids and their salts was conducted. With the help of modern physico-chemical methods: elemental analysis, IR, 1H-NMR-spectroscopy the structure of synthesized compounds, and their individuality by HPLC-MS is proved. In the IR spectrum of the compound 2-(4-phenyl-5-(thiophene-2-ylmethyl)-4H-1,2,4-triazole-3-ylthio)acetate acid Ic available band fluctuations groups characteristic for the nucleus of 1,2,4-triazole: NH– in the range of 3 400–3 100 cm-1,–C=N– – 1 690–1 620 cm-1. Also present band fluctuations groups –C–S– at 691 cm-1. Available band fluctuations characteristic of the group –CH2 within 1496.59 cm-1 and group –COO-H– – 1722.70 cm-1. This suggests the possibility to further study the biological action of the synthesized compounds.
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