A series of 2-substituted isothiazolo[5,4-b]pyridine-3(2H)-thiones isothiazolo[5,4-b]pyridin-3(2H)-ones, N-substituted 2-sulfanylnicotinamides and the corresponding carbothioamide derivatives were synthesized and evaluated for their antimicrobial activity against several strains of Gram + and Gram - bacteria and fungi. Chemical syntheses were resumed into a comprehensive cyclic route that enables the reversible conversion for each derivative of the series considered. Among the tested compounds the N-(aralkyl)-2-sulfanylnicotinamides show the highest fungitoxicity (MIC = 1.25-5 mug/ml). The best activity towards Gram-positive bacteria was in the range of 2.5-5 mug/ml. Activity against Gram-negative bacteria was generally very poor for all compounds.

3H-[1,2]Dithiolo[3,4-b]pyridine-3-thione and its derivatives. Synthesis and antimicrobial activity

PREGNOLATO, MASSIMO
;
TERRENI, MARCO;UBIALI, DANIELA;PAGANI, GIUSEPPE;BORGNA, PIETRO;
2000-01-01

Abstract

A series of 2-substituted isothiazolo[5,4-b]pyridine-3(2H)-thiones isothiazolo[5,4-b]pyridin-3(2H)-ones, N-substituted 2-sulfanylnicotinamides and the corresponding carbothioamide derivatives were synthesized and evaluated for their antimicrobial activity against several strains of Gram + and Gram - bacteria and fungi. Chemical syntheses were resumed into a comprehensive cyclic route that enables the reversible conversion for each derivative of the series considered. Among the tested compounds the N-(aralkyl)-2-sulfanylnicotinamides show the highest fungitoxicity (MIC = 1.25-5 mug/ml). The best activity towards Gram-positive bacteria was in the range of 2.5-5 mug/ml. Activity against Gram-negative bacteria was generally very poor for all compounds.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11571/133247
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