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Med Chem ; 14(3): 311-319, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29032761

RESUMO

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.


Assuntos
Antibacterianos/farmacologia , Imidazóis/farmacologia , Tiazóis/farmacologia , Antibacterianos/síntese química , Antifúngicos/síntese química , Antifúngicos/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Bifidobacterium/efeitos dos fármacos , Econazol/farmacologia , Células HeLa , Humanos , Imidazóis/síntese química , Lactobacillus/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Tiazóis/síntese química , Sistema Urogenital/microbiologia
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