TDAE-assisted synthesis of new imidazo[2,1- b ]thiazole derivatives as anti-infectious agents
作者:Thierry Juspin、Michèle Laget、Thierry Terme、Nadine Azas、Patrice Vanelle
DOI:10.1016/j.ejmech.2009.10.048
日期:2010.2
A series of new imidazo[2,1-b]thiazoles was prepared in moderate to good yields in a four step synthesis using the TDAE methodology from 6-chloromethyl-5-nitroimidazo[2,1-b]thiazole and keto esters, ketomalonates and ketolactams. All compounds were tested for their antibacterial and antifungal activities against four bacterial strains (two Gram positive and two Gram negative ones) and four yeasts.
一系列新的咪唑并[2,1- b是在中度使用TDAE方法从6-氯甲基-5-硝基咪唑并[2,1-制备在四步合成法良好的产率]噻唑b ]噻唑和酮酯,ketomalonates和酮内酰胺。 测试了所有化合物对四种细菌菌株(两种革兰氏阳性和两种革兰氏阴性)和四种酵母菌的抗菌和抗真菌活性。在这些合成的5-硝基咪唑并[2,1- b ]噻唑类化合物中,化合物1和6对所有念珠菌菌株均显示出有效的抗菌活性,而化合物3e对热带念珠菌显示出有趣的抗真菌潜力。