Novel N-(1-thia-4-azaspiro[4.5]decan-4-yl)carboxamide derivatives as potent and selective influenza virus fusion inhibitors.

Hemagglutinin is the surface protein of the influenza virus that mediates both binding and penetration of the virus into host cells. We here report on the synthesis and structure-activity relationship of some novel N-(1-thia-4-azaspiro[4.5]decan-4-yl)-carboxamide compounds carrying the 5-chloro-2-methoxybenzamide structure, designed as influenza virus fusion inhibitors.

Synthesis and anti-coronavirus activity of a series of 1-thia-4-azaspiro[4.5]decan-3-one derivatives.

A series of 1-thia-4-azaspiro[4.5]decan-3-ones bearing an amide group at C-4 and various substitutions at C-2 and C-8 were synthesized and evaluated against human coronavirus and influenza virus. Compounds 7m, 7n, 8k, 8l, 8m, 8n, and 8p were found to inhibit human coronavirus 229E replication.

Microwave assisted synthesis and anti-influenza virus activity of 1-adamantyl substituted N-(1-thia-4-azaspiro[4.5]decan-4-yl)carboxamide derivatives.

A microwave-assisted three-component one-pot cyclocondensation method was applied for the synthesis of novel N-(1-thia-4-azaspiro[4.5]decan-4-yl)carboxamide compounds carrying an adamantyl moiety. The structures of the compounds were confirmed by spectral and elemental analysis.

Synthesis and Biological Evaluation of some new Imidazo[1,2-a]pyridines.

A series of new 1-[(2,8-dimethylimidazo[1,2-a]pyridine-3-yl)carbonyl]-4-alkyl/arylthiosemicarbazides, 2-[(2,8-dimethylimidazo[1,2-a]pyridine-3-yl)carbonyl]hydrazono-3-alkyl thiazolidin-4-ones, 2-(2,8-dimethylimidazo[1,2-a]pyridine-3-yl)-5-arylamino-1,3,4-oxadiazoles and 4-alkyl/aryl-2,4-dihydro-5-(2,8-dimethylimidazo[1,2-a]pyridine-3-yl)-3H-1,2,4-triazole-3-thiones were synthesized. The structures of the compounds have been elucidated by IR, 1H NMR, EI mass spectra and elemental analysis. Antibacterial, antifungal and antimycobacterial activities of compounds were evaluated against various microorganisms and some of them were found to be active in varying degrees against Staphylococcus aureus, Staphylococcus epidermidis or Mycobacterium tuberculosis H37Rv.

Novel inhibitors of influenza virus fusion: structure-activity relationship and interaction with the viral hemagglutinin.

A new class of N-(1-thia-4-azaspiro[4.5]decan-4-yl)carboxamide inhibitors of influenza virus hemagglutinin (HA)-mediated membrane fusion that has a narrow and defined structure-activity relationship was identified. In Madin-Darby canine kidney (MDCK) cells infected with different strains of human influenza virus A/H3N2, the lead compound, 4c, displayed a 50% effective concentration of 3 to 23 muM and an antiviral selectivity index of 10.

2-[(1,5-Dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)amino]-1-methyl-2-oxoethyl pyrrolidine-1-carbodithio-ate.

In the title compound, C(19)H(24)N(4)O(2)S(2), inversion-related mol-ecules are linked together to form a dimer by N-H⋯O and C-H⋯O hydrogen bonds, generating two R(2) (1)(6) rings and one R(2) (2)(10) ring motif. An inter-molecular C-H⋯O hydrogen bond connects the dimers to each other. An intra-molecular C-H⋯O inter-action occurs.

Synthesis of some new 6-methylimidazo[2,1-b]thiazole-5-carbohydrazide derivatives and their antimicrobial activities.

In this study, 14 new compounds having 6-methyl-N2-(alkylidene/cycloalkylidene)imidazo[2,1-b]thiazole-5-carbohydrazide (3a-g), 3-[[(6-methylimidazo[2,1-b]thiazole-5-yl)carbonyl]amino]-4-thiazolidinone (4a-d) and 4-[[(6-methylimidazo[2,1-b]thiazole-5-yl)carbonyl]amino]-1-thia-4-azaspiro[4.4]nonan/[4.5]decan-3-one (4e-g) structures were synthesized.

LC determination of aminoglutethimide enantiomers as dansyl and fluorescamine derivatives in tablet formulations.

Determination of dansyl (AG-DNS) and fluorescamine (AG-F) derivatives of rac-aminoglutethimide in tablet formulation by HPLC has been achieved on a cellulose tris-(3,5-dimethylphenyl carbamate), known as Chiralcel OD and OD-R under normal and reversed phase columns, respectively, using a fluorescence detector (lambda(ex), 360 nm; lambda(em), 530 nm for AG-DNS derivatives; lambda(ex), 395 nm, lambda(em), 495 nm for fluorescamine derivatives (AG-F)). The best results were obtained with mobile phase ethanol:cyclohexane:methanol (95:5:2 v/v/v) for AG-DNS derivatives and acetonitrile:0.5% ortho-phosphoric acid (85:15 v/v) containing 0.