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Title: Synthesis and evaluation of novel azoles as potent antifungal agents. Author: Li L, Ding H, Wang B, Yu S, Zou Y, Chai X, Wu Q. Journal: Bioorg Med Chem Lett; 2014 Jan 01; 24(1):192-4. PubMed ID: 24332489. 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.[Abstract] [Full Text] [Related] [New Search]