ABSTRACT
In this study, a series of phenylethylsulfanyl-1,3-thiazolo-thiazolidine-2,4-dione derivatives (VII a-f, VIII a-f) and 5-methyl-[1,2,4]triazolyl-sulfanyl-1,3-thiazolo-thiazolidine-2,4-dione derivatives (IX a-f, X a-f) were synthesized and evaluated for their antibacterial and antifungal activities against S. aureus (ATCC 25923), methicillin resistant S. aureus (MRSA ATCC 43300), B. subtilis (ATCC 6633), E. coli (ATCC 23556) and C. albicans (ATCC10145). All the compounds were found active against used bacteria.
Subject(s)
Anti-Infective Agents/chemical synthesis , Anti-Infective Agents/pharmacology , Bacteria/drug effects , Thiazolidinediones/chemical synthesis , Thiazolidinediones/pharmacology , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/pharmacology , Antifungal Agents/chemical synthesis , Antifungal Agents/pharmacology , Bacillus subtilis/drug effects , Candida albicans/drug effects , Escherichia coli/drug effects , Methicillin-Resistant Staphylococcus aureus/drug effects , Microbial Sensitivity Tests , Staphylococcus aureus/drug effects , Structure-Activity RelationshipABSTRACT
In this study, a series of thiazolyl-2,4-thiazolidinediones (VIa-f, VIHa-f and VIIa-f) was prepared by Knoevenagel reaction of substituted phenacyl-2,4-thiazolidinediones (IVa-f)/substituted benzyl-2,4-thiazolidinediones (Va-f) with chlorothiazolecarbaldehydes (II, III). The prepared compounds were tested for their insulinotropic activities in INS-1 cells. A significant insulinotropic effect was seen with compounds VIa, VIb, VIe, VIIa, VIIb and VIIId. Introducing a 2-[(phenylethyl)thio] group into the thiazole ring increased the biological effect, whereas NO2 groups in phenylacyl or benzyl groups diminished the effects.
Subject(s)
Hypoglycemic Agents/chemical synthesis , Hypoglycemic Agents/pharmacology , Thiazolidinediones/chemical synthesis , Thiazolidinediones/pharmacology , Animals , Cells, Cultured , Glucose/pharmacology , Indicators and Reagents , Insulin/metabolism , RatsABSTRACT
In this study, a series of thiazolyl thiazolidine-2,4-dione derivatives (Va-f and VIa-f) were synthesized and evaluated for their antibacterial and antifungal activities against Staphylococcus aureus (ATCC 25923), methicillin resistant S. aureus (MRSA ATCC 43300), methicillin resistant S. aureus (MRSA isolate), and Escherichia coli (ATCC 23556) and C. albicans (ATCC10145). All the compounds were found active against used microorganisms.
