Výsledky vyhledávání - "Madina G. Kadieva"

Antagonists of Serotonin 5-HT6 Receptors. VI. Substituted 3-(Phenylsulfonyl)Quinolines, Synthesis and Structure–Activity Relationships

Autor: E. S. Golovina, Alexandre Vasilievich Ivachtchenko, Oleg D. Mitkin, Ilya Okun, Madina G. Kadieva

Publikováno v: Pharmaceutical Chemistry Journal. 48:646-660

In continuation of research and development of new high-efficacy drugs based on 5-HT6 receptor antagonists for the treatment of CNS disorders, we synthesized a series of new 3-(phenylsulfonyl)quinoline derivatives, performed their molecular docking,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::86cfd7cb7234c903cea12913820d26a0
https://doi.org/10.1007/s11094-015-1164-5

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Synthesis of substituted diphenyl sulfones and their structure–activity relationship with the antagonism of 5-НТ6 receptors

Autor: Ilya Okun, Oleg D. Mitkin, Madina G. Kadieva, S. E. Tkachenko, Elena S. Golovina, Alexandre V. Ivachtchenko

Publikováno v: Bioorganic & Medicinal Chemistry. 21:4614-4627

Substituted diphenyl sulfones (10a–n) were synthesised, and the structures were confirmed by NMR, LC–MS and X-ray crystallography. Their antagonistic activities towards 5-HT6 receptor were assessed in a cell-based functional assay. Diphenyl sulfo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e08f5b2180dfe9917ccadbf4f5d8ce9
https://doi.org/10.1016/j.bmc.2013.05.040

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Antagonists of serotonin 5-HT6 receptors. iv. synthesis and structure-activity interactions in amines containing the 3-(arylsulfonyl)-2-(methylthio)pyrazolo[1,5-a]pyrimidine fragment

Autor: Madina G. Kadieva, V. M. Kysil, Oleg D. Mitkin, E. S. Golovina, Alexandre Vasilievich Ivachtchenko

Publikováno v: Pharmaceutical Chemistry Journal. 46:595-602

New 3-(arylsulfonyl)-2-(methylthio)pyrazolo[1,5-a]pyrimidines with a substituent amino group in the 7 position were synthesized and their 5-HT6 antagonist activity was studied. The transition from 7-amino and 7-dimethylamino derivatives to 7-aminoalk

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https://doi.org/10.1007/s11094-013-0853-1

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Antagonists of serotonin 5-HT6 receptors. III. Pyridine-substituted 3-(phenylsulfonyl)pyrazolo[1,5-a]pyrimidines: synthesis and structure – activity relationship

Autor: Madina G. Kadieva, A. V. Ivashchenko, Oleg D. Mitkin, Ilya Okun, E. S. Golovina, V. M. Kysil

Publikováno v: Pharmaceutical Chemistry Journal. 46:406-410

In continuation of studies on 3-(phenylsulfonyl)pyrazolo[1,5-a]pyrimidine derivatives as 5-HT6 receptor antagonists, new compounds with a pyridine moiety in the 5-and/or 7-position were obtained and their antagonistic activity was screened. It was es

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e82b1f0df988bde2df00cbf6445c8e26
https://doi.org/10.1007/s11094-012-0810-4

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Serotonin 5-HT6 receptor antagonists. II. Synthesis and structure—activity relationship of 3-arylsulfonyl-2-methylthiopyrazolo[1,5-a]pyrimidines with substituents containing an amine in the 6-position

Autor: V. M. Kysil, Ilya Okun, E. S. Golovina, Madina G. Kadieva, Alexandre Vasilievich Ivachtchenko, Oleg D. Mitkin

Publikováno v: Pharmaceutical Chemistry Journal. 46:337-345

3-(Arylsulfonyl)-2-(methylthio)pyrazolo[1,5-a]pyrimidines containing substituents with an amine in the 6-position were synthesized. Their structure—activity (antagonist) relationship was studied with respect to serotonin 5-HT6 receptors. It was sho

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::d68b54afcf7e08120194ad83ca3a08e0
https://doi.org/10.1007/s11094-012-0794-0

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5-HT6 Receptor antagonists. I. Screening of the library of various heterocyclic compounds containing an alkylsulfonyl moiety

Autor: Sergey E. Tkachenko, Madina G. Kadieva, Alexandre Vasilievich Ivachtchenko, Ilya Okun, Oleg D. Mitkin, E. S. Golovina

Publikováno v: Pharmaceutical Chemistry Journal. 46:274-284

High-throughput screening of a specific set (focused library) of heterocyclic compounds containing an alkylsulfonyl moiety (a total of 2827 compounds from 78 combinatorial libraries) was performed in order to discover highly effective 5-HT6 receptor

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::81b1fbbc17f37da07f481720def79c6c
https://doi.org/10.1007/s11094-012-0779-z

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Antagonists of 5-HT6 receptors. Substituted 3-(phenylsulfonyl)pyrazolo[1,5-a]pyrido[3,4-e]pyrimidines and 3-(phenylsulfonyl)pyrazolo[1,5-a]pyrido[4,3-d]pyrimidines—Synthesis and ‘structure–activity’ relationship

Autor: Alexandre V. Ivachtchenko, Madina G. Kadieva, Volodymyr M. Kysil, Oleg D. Mitkin, Anton A. Vorobiev, Ilya Okun, Elena S. Golovina

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:4273-4280

Synthesis and biological evaluation of a new series of structurally unrestricted and intramolecular hydrogen bond restricted derivatives of 3-(phenylsulfonyl)pyrazolo[1,5- a ]pyrido[3,4- e ]pyrimidines (angular tricyclics) and 3-(phenylsulfonyl)pyraz

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::7847abf41214982b2b457c63a344d9f6
https://doi.org/10.1016/j.bmcl.2012.05.036

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Synthesis and Structure–Activity Relationship (SAR) of (5,7-Disubstituted 3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidin-2-yl)-methylamines as Potent Serotonin 5-HT6 Receptor (5-HT6R) Antagonists

Autor: Madina G. Kadieva, Sergey E. Tkachenko, Elena S. Golovina, Volodymyr M. Kysil, Alexandre V. Ivachtchenko, Oleg D. Mitkin, Ilya Okun

Publikováno v: Journal of Medicinal Chemistry. 54:8161-8173

Syntheses, biological evaluation as 5-HT(6) receptor (5-HT(6)R) antagonists, and structure-activity relationships for a series of novel 5,7-disubstituted (3-arylsulfonyl-pyrazolo[1,5-a]pyrimidins are disclosed. The molecule conformational flexibility

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c3c7bc2dbec27c5eb42f6d4cfa6acc65
https://doi.org/10.1021/jm201079g

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2-Substituted 5,6-dimethyl-3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidines: New series of highly potent and specific serotonin 5-HT6 receptor antagonists

Autor: Ilya Okun, Elena S. Golovina, Madina G. Kadieva, Volodymyr M. Kysil, Sergey E. Tkachenko, Angela G. Koryakova, Oleg D. Mitkin, Alexandre V. Ivachtchenko

Publikováno v: European Journal of Medicinal Chemistry. 46:1189-1197

Syntheses, biological evaluation, and structure-activity relationships for a series of novel 2-substituted 3-benzenesulfonyl-5,6-dimethyl-pyrazolo[1,5-a]pyrimidines are disclosed. In spite of a wide, four orders of magnitude, SAR range (K(i) varied f

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::43e18085bfd44c2bf6c8d83ef4722bf1
https://doi.org/10.1016/j.ejmech.2011.01.038

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Synthesis and biological study of 3-(phenylsulfonyl)thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidines as potent and selective serotonin 5-HT6 receptor antagonists

Autor: Madina G. Kadieva, Sergiy M. Kovalenko, Sergey E. Tkachenko, Irina M. Ravnyeyko, Elena S. Golovina, Oleg D. Mitkin, Ilya Okun, Oleg V. Zaremba, Alexandre V. Ivachtchenko, Angela G. Koryakova

Publikováno v: Bioorganic & Medicinal Chemistry. 18:5282-5290

A number of 3-(phenylsulfonyl)thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidines were prepared and their 5-HT6 receptor binding affinity and ability to inhibit the functional cellular responses to serotonin were evaluated. 3-[(3-Chlorophenyl)sulfonyl]-N-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f9885c12940216d8379c0ad034f43139
https://doi.org/10.1016/j.bmc.2010.05.051

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