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Investigation on the Effects of Antimicrobial imidazo[2,1-b]thiazole Derivatives on the Genitourinary Microflora.
Medicinal Chemistry ( IF 1.9 ) Pub Date : 2017-10-17 , DOI: 10.2174/1573406413666171010110819
Rita Morigi 1 , Beatrice Vitali 1 , Cecilia Prata 1 , Rogers A N Palomino 1 , Alessandra Graziadio 1 , Alessandra Locatelli 1 , Mirella Rambaldi 1 , Alberto Leoni 1
Affiliation  

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.

中文翻译:

抗菌咪唑并[2,1-b]噻唑衍生物对泌尿生殖道菌群的影响研究。

背景技术含有桥头氮原子的稠合五元杂环由于其不同的生物活性而在药物化学领域中特别有用。其中,咪唑并[2,1-b]噻唑是一种引人注目的稠合杂环核,已得到广泛研究。目的本研究的目的是研究咪唑并[2,1-b]噻唑衍生物作为抗菌剂治疗泌尿生殖道感染的治疗应用。方法采用传统的合成方法来获得少量的咪唑并噻唑衍生物。结果在此,我们报道了咪唑并[2,1-b]噻唑或咪唑并[2,1-b]噻唑烷衍生物对选定的真菌,革兰氏阳性和革兰氏阴性细菌的抗菌活性。而且,进行实验以研究对内生微生物的干扰。结论该系列中最有趣的是硫氰基衍生物(19,23),其在泌尿生殖道感染的治疗中表现出良好的特性:涵盖细菌和真菌的一系列活性,以及​​与抵抗病原体的乳杆菌相比,其对关键系的影响降低。
更新日期:2019-11-01
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