title: Synthesis and evaluation of novel azoles as potent antifungal agents.
abstract: Using a rational approach to the design of antifungal agents, a series of azole agents with 1,3,4-oxadiazole side chains were designed and synthesized. The results of preliminary in vitro antifungal tests with eight human pathogenic compounds showed that all of the title compounds exhibited excellent activities against all of the tested fungi except Aspergillus fumigatus. Compounds 11e and 11f were found to be the most effective, with a minimum inhibitory concentration of 0.0039μg/mL, followed by voriconazole, which has a MIC of 0.0625μg/mL. The 1,3,4-oxadiazole side chain is not the major contributor but plays a role in eliciting the observed antifungal activity.
authors: Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China; Cadet Company 2nd, Faculty of Naval Medicine, Second Military Medical University, 800 Xiangyin Road, Shanghai 200433, China.
authors: Liangjing
authors: L
authors: Li
authors: Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China.
authors: Hao
authors: H
authors: Ding
authors: Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China.
authors: Baogang
authors: B
authors: Wang
authors: Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China.
authors: Shichong
authors: S
authors: Yu
authors: Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China.
authors: Yan
authors: Y
authors: Zou
authors: Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China. Electronic address: chaixy1207@163.com.
authors: Xiaoyun
authors: X
authors: Chai
authors: Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China. Electronic address: wuqy640319@163.com.
authors: Qiuye
authors: Q
authors: Wu
mesh_terms: D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001393:Azoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D005658:Fungi / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000935:Antifungal Agents; D001393:Azoles
keywords: Antifungal activity; Azole; Synthesis