Search Results - "Mitkin, Oleg D"
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Synthesis, X-Ray Crystal Structure, Hirshfeld Surface Analysis, and Molecular Docking Study of Novel Hepatitis B (HBV) Inhibitor: 8-Fluoro-5-(4-fluorobenzyl)-3-(2-methoxybenzyl)-3,5-dihydro-4H-pyrimido[5,4-b]indol-4-one
Published in Crystals (Basel) (01-08-2019)“…A method for the synthesis of 8-fluoro-5-(4-fluorobenzyl)-3-(2-methoxybenzyl)-3,5-dihydro-4H-pyrimido[5,4-b]indol-4-one has been developed and the electronic…”
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Novel One-Pot Synthesis of Methyl 4-Hydroxy-2-thioxo-1,2-dihydroquinoline-3-carboxylate: Synthetic and Crystallographic Studies
Published in MolBank (01-12-2019)“…A new suitable method of synthesis of methyl 4-hydroxy-2-thioxo-1,2-dihydroquinoline-3-carboxylate by condensation of methyl 2-isothiocyanatobenzoate and…”
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Synthesis, X-ray crystal structure, Hirshfeld surface analysis, and molecular docking study of novel inhibitor of hepatitis B: methyl 4-fluoro-3-(morpholinosulfonyl)benzo[b]thiophene-2-carboxylate
Published in Heliyon (01-11-2019)“…A method of 4-fluoro-3-(morpholinosulfonyl)benzo[b]thiophene-2-carboxylate synthesis has been developed and the electronic and spatial structure of a new…”
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Photoactive Barbiturate Receptors: An Ultimate Lock-and-Key System in Which the Key Unlocks the Lock
Published in Organic letters (15-03-2007)“…Conditional photofragmentation is achieved with binary systems incorporating the isophthaloyl bis-aminopyridine barbiturate recognition motif and dithiane- or…”
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Non-rigid Diarylmethyl Analogs of Baloxavir as Cap-Dependent Endonuclease Inhibitors of Influenza Viruses
Published in Journal of medicinal chemistry (10-09-2020)“…4-Substituted 2,4-dioxobutanoic acids inhibit influenza virus cap-dependent endonuclease (CEN) activity. Baloxavir marboxil, 4, is approved for treating…”
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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
Published in Journal of medicinal chemistry (08-12-2011)“…Syntheses, biological evaluation as 5-HT6 receptor (5-HT6R) antagonists, and structure–activity relationships for a series of novel 5,7-disubstituted…”
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Synthesis, inhibitory activity and oral dosing formulation of AV5124, the structural analogue of influenza virus endonuclease inhibitor baloxavir
Published in Journal of antimicrobial chemotherapy (12-03-2021)“…Abstract Background The development and clinical implementation of the cap-dependent endonuclease (CEN) inhibitor baloxavir marboxil was a breakthrough in…”
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Synthesis, biological evaluation and in silico modeling of novel integrase strand transfer inhibitors (INSTIs)
Published in European journal of medicinal chemistry (01-03-2020)“…Although a relatively wide range of therapeutic options is currently available for the treatment of HIV/AIDS, it is still among the most serious and virulent…”
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Synthesis, biological evaluation and in silico modeling of novel pan-genotypic NS5A inhibitors
Published in Bioorganic & medicinal chemistry (15-10-2020)“…[Display omitted] •Novel picomolar pan-genotypic NS5A inhibitors.•Combinatorial synthesis, biological evaluation and in silico modeling.•Lead compound showed…”
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Safety and efficacy of aviandr in patients with generalized anxiety disorder: A multicenter, randomized, double-blind, placebo-controlled, dose-finding, pilot study
Published in Journal of psychiatric research (01-11-2021)“…Generalized anxiety disorder (GAD) is associated with an imbalance in the functioning of the stimulating neurotransmitter systems in human's brain. We studied…”
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(3-Phenylsulfonylcycloalkano[e and d]pyrazolo[1,5-a]pyrimidin-2-yl)amines: Potent and Selective Antagonists of the Serotonin 5-HT6 Receptor
Published in Journal of medicinal chemistry (22-07-2010)“…5-HT6 receptors are exclusively localized in the CNS and have high affinity with many psychotropic agents. Though the role of this receptor in many CNS…”
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Design, synthesis and biological evaluation of novel 5-oxo-2-thioxoimidazolidine derivatives as potent androgen receptor antagonists
Published in European journal of medicinal chemistry (24-06-2015)“…A series of novel highly active androgen receptor (AR) antagonists containing…”
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Novel oral anti-influenza drug candidate AV5080
Published in Journal of antimicrobial chemotherapy (01-07-2014)“…Development of a novel drug candidate with improved potency against influenza virus neuraminidase compared with currently available therapeutics, and high…”
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Synthesis and SAR of 3-arylsulfonyl-pyrazolo[1,5-a]pyrimidines as potent serotonin 5-HT6 receptor antagonists
Published in Bioorganic & medicinal chemistry (15-02-2011)“…Syntheses of a series of novel 3-sulfonyl-pyrazolo[1,5-a]pyrimidines and their 5-HT6 receptor antagonistic structure–activity relationship are disclosed. The…”
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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
Published in Bioorganic & medicinal chemistry letters (01-07-2012)“…Synthesis and biological evaluation of a new series of structurally unrestricted and intramolecular hydrogen bond restricted derivatives of…”
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Discovery of Novel Highly Potent Hepatitis C Virus NS5A Inhibitor (AV4025)
Published in Journal of medicinal chemistry (25-09-2014)“…A series of next in class small-molecule hepatitis C virus (HCV) NS5A inhibitors with picomolar potency containing…”
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Crystal structure, Hirshfeld analysis and a molecular docking study of a new inhibitor of the Hepatitis B virus (HBV): ethyl 5-methyl-1,1-dioxo-2-{[5-(pentan-3-yl)-1,2,4-oxadiazol-3-yl]methyl}-2H-1,2,6-thiadiazine-4-carboxylate
Published in Acta crystallographica. Section E, Crystallographic communications (01-01-2020)“…The title compound, C15H22N4O5S, was prepared via alkylation of 3-(chloromethyl)-5-(pentan-3-yl)-1,2,4-oxadiazole in anhydrous dioxane in the presence of…”
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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
Published in European journal of medicinal chemistry (01-04-2011)“…Syntheses, biological evaluation, and structure-activity relationships for a series of novel 2-substituted…”
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Crystal structure, Hirshfeld analysis and a mol-ecular docking study of a new inhibitor of the Hepatitis B virus (HBV): ethyl 5-methyl-1,1-dioxo-2-{[5-(pentan-3-yl)-1,2,4-oxa-diazol-3-yl]meth-yl}-2H-1,2,6-thia-diazine-4-carboxyl-ate
Published in Acta crystallographica. Section E, Crystallographic communications (01-01-2020)“…The title compound, C15H22N4O5S, was prepared via alkyl-ation of 3-(chloro-meth-yl)-5-(pentan-3-yl)-1,2,4-oxa-diazole in anhydrous dioxane in the presence of…”
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A novel influenza virus neuraminidase inhibitor AV5027
Published in Antiviral research (01-12-2013)“…•Novel small-molecule neuraminidase inhibitors from a combinatorial approach.•One NA inhibitor revealed picomolar potency in enzymatic and cell-based…”
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