Rita Morigi1, Beatrice Vitali1, Cecilia Prata1, Rogers A N Palomino1, Alessandra Graziadio1, Alessandra Locatelli1, Mirella Rambaldi1, Alberto Leoni1.
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. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.
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. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.
Entities:
Keywords:
imidazo[2, 1-b]thiazole; Ampicillin; antiproliferative effects; bifidobacteria; lactobacilli; urogenital pathogens
Mesh：
Substances：
Year: 2018
PMID： 29032761 DOI： 10.2174/1573406413666171010110819
Source DB: PubMed Journal: Med Chem ISSN： 1573-4064 Impact factor: 2.745