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Med Chem ; 14(3): 311-319, 2018.
Article in English | MEDLINE | ID: mdl-29032761

ABSTRACT

BACKGROUND: Fused five-membered heterocyclic rings containing bridgehead nitrogen atom are particularly versatile in the field of medicinal chemistry because of their different biological activities. Among them, the imidazo[2,1-b]thiazole is an attractive fused heterocyclic core that has been extensively studied. OBJECTIVE: The aim of the current study was to study the therapeutic applications of imidazo[2,1- b]thiazole derivatives as antimicrobial agents for the treatment of genitourinary infections. METHOD: A traditional synthetic methodology was involved to obtain a small series of imidazothiazole derivatives. RESULTS: Herein, we report the antimicrobial activity of the imidazo[2,1-b]thiazole or imidazo[2,1- b]thiazolidine derivatives against selected fungi, Gram-positive and Gram-negative bacteria. Moreover, experiments were carried out to investigate the interference towards the endogenous microbiota. CONCLUSION: The most interesting of the series are the thiocyano derivatives (19, 23) showing a good profile for the treatment of genitourinary infections: a spectrum of activity covering both bacteria and fungi together with a reduced impact versus critical lines of Lactobacillus exerting defense against pathogens.


Subject(s)
Anti-Bacterial Agents/pharmacology , Imidazoles/pharmacology , Thiazoles/pharmacology , Anti-Bacterial Agents/chemical synthesis , Antifungal Agents/chemical synthesis , Antifungal Agents/pharmacology , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/pharmacology , Bifidobacterium/drug effects , Econazole/pharmacology , HeLa Cells , Humans , Imidazoles/chemical synthesis , Lactobacillus/drug effects , Microbial Sensitivity Tests , Thiazoles/chemical synthesis , Urogenital System/microbiology
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