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Title of Journal: Arch Pharm Res

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Abbravation: Archives of Pharmacal Research

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Publisher

Pharmaceutical Society of Korea

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DOI

10.1006/mgme.1998.2701

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ISSN

1976-3786

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Synthesis and biological evaluation of novel fluco

Authors: Jun Liao Fan Yang Lei Zhang Xiaoyun Chai Qingjie Zhao Shichong Yu Yan Zou Qingguo Meng Qiuye Wu
Publish Date: 2014/05/17
Volume: 38, Issue: 4, Pages: 470-479
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Abstract

A novel series of fluconazole based mimics incorporating 134oxadiazole moiety were designed and synthesized All the title compounds were characterized by 1HNMR 13CNMR and QTOFMS Preliminary results revealed that most of analogues exhibited significant antifungal activity against seven pathogenic fungi Compounds 9g and 9k MIC80 ≤ 0125 μg/mL respectively were found more potent than the positive controls itraconazole and fluconazole as broadspectrum antifungal agents The observed docking results showed that the 134oxadiazole moiety enhanced the affinity binding to the cytochrome P450 14αdemethylase CYP51

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