In this study, a series of phenylefhylsul-fanyl-1,3-thiazolo-thiazolidine-2,4-dione derivatives (VII a ?f, VIII a?f) and 5-methyl-[1,2,4] triazolyl-sulfanyl-1,3-fhia-zolo-thiazolidine-2,4-dione derivatives (IXa?f, Xa?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.
ones. -The products (V) are tested for their insulinotropic activities in INS-1 cells. Introducing a phenylethylthio group in the thiazole ring increases the activity, whereas NO2 substituents in the phenacyl or benzyl moiety diminish the biological effect. The SAR is discussed. -(BOZDAG-DUENDAR*, O.; MENTESE, A.; VERSPOHL, E. J.; Arzneim.-Forsch. 58 (2008) 3, 131-135; Dep. Pharm. Chem., Fac. Pharm., Ankara Univ., TR-06100 Ankara, Turk.; Eng.) -H. Haber 29-129
Summary
In this study, a series of thiazolyl-2,4-thi-azolidinediones (VIa-f, VIIa-f and VIIIa-f) was prepared by Knoevenagel reaction of substituted phenacyl-2,4-thiazolidine-diones (IVa-f)/substituted benzyl-2,4-thi-azolidinediones (Va-f) with chlorothiaz-olecarbaldehydes (II, III). The prepared compounds were tested for their insuli-notropic 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 N02 groups in phenylacyl or benzyl groups diminished the effects.
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