Chinese Journal of Applied Chemistry ›› 2015, Vol. 32 ›› Issue (1): 43-52.DOI: 10.11944/j.issn.1000-0518.2015.01.140094

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

CHEN Yong*, WU Hankui, LONG Junfei   

  1. Chemistry & Chemical Industry School,Anyang Normal University,Anyang,He'nan 455000,China
  • Received:2014-03-25 Revised:2014-07-11 Published:2015-01-06 Online:2015-01-06
  • Contact: Corresponding author:CHEN Yong, professor; E-mail:chenqiaoyong@aliyun.com; Research interests:organic(drug) synthesis and organic functional material

Abstract:

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.

Key words: dihalobiphenyl, synthesis, novel azole derivatives, antifungal activity

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