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

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。

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

Novel azole title compounds with 2',4'-dihalobiphenyl 3a~3k were synthesized via F-C acylation, reduction and substitution reactions starting from 2,4-dihalobiphenyl. The structures of these compounds were confirmed by IR, ¹H NMR, ¹³C NMR and HMRS spectra. In vitro antifungal 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. Antifungal 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.