21 research outputs found

    4-Benzyl-8-phenyl-1-thia-4-aza­spiro­[4.5]decan-3-one

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    In the title compound, C21H23NOS, the thia­zolidine ring adopts a twist conformation about one of its C—S bonds, while the cyclo­hexane ring has a chair conformation. The S and N atoms attached to the spiro C atom are in axial and equatorial orientations, respectively. The thia­zolidine ring forms dihedral angles of 86.24 (14) and 31.82 (15)° with the directly attached and remote terminal benzene rings, respectively. The dihedral angle between the two terminal benzene rings is 86.74 (14)°. In the crystal, the only significant directional inter­action is a weak C—H⋯π bond, which generates [010] chains

    Fused Heterocycles: Synthesis of Some New Imidazo[1,2-a]- pyridine Derivatives

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    Some new thiazolidines and spirothiazolidines derived from hydrazones of2-methylimidazo[1,2-a]pyridine-3-carboxylic acid hydrazide, a bioisosteric derivative ofisoniazid, were synthesized and characterized by analytical, IR, 1H- and 13C-NMR andmass spectral data. Some of the newly synthesized compounds were screened for theirantimycobacterial activities. None of the tested compounds showed significant in vitroantituberculous activity at 6.25 μg/mL (MIC rifampin 0.031 μg/mL)

    Fused heterocycles: Synthesis of some new imidazopyridines as anti-mycobacterial agents

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    The reaction of semicarbazones bearing an imidazo[ 1,2-a] pyridine ring system with mercaptoacetic acid was investigated. The anti-mycobacterial activity of the compounds thus obtained were evaluated against Mycobacterium tuberculosis H(37)Rv, using rifampin as the standard. Only IVe showed activity at 6.25 mu g mL(-1)

    Fused Heterocycles: Synthesis of Some New Imidazo[1,2-a]- pyridine Derivatives

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    Some new thiazolidines and spirothiazolidines derived from hydrazones of2-methylimidazo[1,2-a]pyridine-3-carboxylic acid hydrazide, a bioisosteric derivative ofisoniazid, were synthesized and characterized by analytical, IR, 1H- and 13C-NMR andmass spectral data. Some of the newly synthesized compounds were screened for theirantimycobacterial activities. None of the tested compounds showed significant in vitroantituberculous activity at 6.25 μg/mL (MIC rifampin 0.031 μg/mL)

    FUSED HETEROCYCLES : SYNTHESIS OF SOME NEW IMIDAZOTHIAZOLES

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    Reaction of aldehyde-hydrazones or semicarbazones bearing an imidazo[2,1-b] [1,3]thiazole ring system with mercaptoalkanoic acids were investigated. Antimycobacterial activities of compounds thus obtained were evaluated against Mycobacterium tuberculosis H37Rv using rifampine as standard

    Fused heterocycles: Synthesis of some new imidazothiazoles

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    Reaction of aldehyde-hydrazones or semicarbazones bearing an imidazo[2,1-b] [1,3]thiazole ring system with mercaptoalkanoic acids were investigated. Antimycobacterial activities of compounds thus obtained were evaluated against Mycobacterium tuberculosis H37Rv using rifampine as standard

    The synthesis of novel pyrazole-3,4-dicarboxamidesbearing 5-amino-1,3,4-thiadiazole-2-sulfonamide moiety with effective inhibitory activity against the isoforms of human cytosolic carbonic anhydrase I and II

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    WOS: 000387978400008PubMed ID: 27454619A series of 1-(3-substituted-phenyl)-5-phenyl-N-3,N-4-bis(5-sulfamoyl-1,3,4-thiadiazol-2-yl)-1H-pyrazole-3,4- dicarboxamides (4-15) were synthesized. The structures of these pyrazole-sulfonamides were confirmed by FT-IR, H-1 NMR, C-13 NMR and elemental analysis methods. Human cytosolic carbonic anhydrase (CA, EC 4.2.1.1) isozymes (hCA I and II) were purified from erythrocyte cells by affinity chromatography. The inhibitory effects of newly synthesized derivatives (4-15) were investigated in vitro on esterase activities of these isozymes. The K-i values were determined as 0.119-3.999 mu M for hCA I and 0.084-0.878 mu Mfor hCA II. The results showed that the compound 6 for hCA I and the compound 11 for hCA II had the highest inhibitory effect. Beside that, the compound 8 had the lowest inhibition effect on both isozymes. (C) 2016 Elsevier Inc. All rights reserved.Dumlupinar University Research FundDumlupinar University [2010/14]This work was supported by the Dumlupinar University Research Fund (Project Number: 2010/14). Also the authors are grateful to the Ataturk University Faculty of Sciences Department of Chemistry for providing the usage of spectroanalytic laboratory facilities and Dumlupinar University Faculty of Arts and Sciences Department of Physics for FT-IR measurements
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