含有2,4-二卤代联苯基的新型唑类衍生物的合成及其抗真菌活性  

Synthesis and Antifungal Activity of Novel Azole Derivatives with 2',4'-Dihalobiphenyl

作　　者：陈勇[1] 吴汉夔[1] 龙俊飞[1] 

机构地区：[1]安阳师范学院化学化工学院,河南安阳455000

出　　处：《应用化学》2015年第1期43-52,共10页Chinese Journal of Applied Chemistry

基　　金：河南省科技攻关立项课题(122102310520);安阳市科技攻关立项课题(编号:20)~~

摘　　要：以2,4-二卤代联苯为原料,经傅-克酰基化、还原、取代等反应步骤,合成了含有2,4-二卤代联苯基的新型唑类目标化合物3a^3k,其结构用红外光谱(IR)、高分辨质谱(HMRS)、核磁共振氢谱(1H NMR)、核磁共振碳谱(13C NMR)等技术手段进行了表征。测试了目标化合物的体外抗真菌活性,结果表明,所有目标化合物对所测试的致病真菌均有一定程度的抗真菌活性。其中化合物3a^3k对红色发癣菌和石膏样毛癣菌的抗真菌活性和两性霉素B相当,化合物3b、3c、3e、3f、3h、3i、3k对白色念珠菌的抗真菌活性优于或等于酮康唑。Novel azole title compounds with 2＇,4＇-dihalobiphenyl 3a reduction and substitution reactions starting from 2,4-dihalobiphenyl. confirmed by 1R, ^1H NMR, ^13C NMR and HMRS spectra. In vitro an - 3k were synthesized via F-C acylation, The structures of these compounds were tifungal activities of title compounds were evaluated. The results of preliminary biological tests show that the title compounds exhibit antifungal activities against to tested pathogenic fungi to some extent. An activities against to Trichophyton rubrum and Trichophyton mentagrophytes of compounds 3a - 3k were equivalent to that of Amphotericin B. Antifungal activities of compounds 3b, 3c, 3e, 3f, 3h, 3i, 3k against to Candiada albicans were higher than that of ketoconazole.

关 键 词：二卤代联苯 合成 新型唑类衍生物 抗真菌活性 

分 类 号：O626[理学—有机化学]