Synthesis and evaluation of novel azoles as potent antifungal agents
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 excellen...
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Published in | Bioorganic & medicinal chemistry letters Vol. 24; no. 1; pp. 192 - 194 |
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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 0.0039 mu g/mL, followed by voriconazole, which has a MIC of 0.0625 mu g/mL. The 1,3,4-oxadiazole side chain is not the major contributor but plays a role in eliciting the observed antifungal activity. (C) 2013 Elsevier Ltd. All rights reserved. |
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AbstractList | 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 0.0039 mu g/mL, followed by voriconazole, which has a MIC of 0.0625 mu g/mL. The 1,3,4-oxadiazole side chain is not the major contributor but plays a role in eliciting the observed antifungal activity. (C) 2013 Elsevier Ltd. All rights reserved. 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. 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 0.0039 mu g/mL, followed by voriconazole, which has a MIC of 0.0625 mu g/mL. The 1,3,4-oxadiazole side chain is not the major contributor but plays a role in eliciting the observed antifungal activity. |
Author | Chai, Xiaoyun Ding, Hao Wang, Baogang Zou, Yan Wu, Qiuye Li, Liangjing Yu, Shichong |
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Keywords | Antifungal activity CASPOFUNGIN Azole Synthesis |
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SubjectTerms | Antifungal Agents - chemical synthesis Antifungal Agents - chemistry Antifungal Agents - pharmacology Aspergillus fumigatus Azoles - chemical synthesis Azoles - chemistry Azoles - pharmacology Chemistry Chemistry, Medicinal Chemistry, Organic Dose-Response Relationship, Drug Fungi - drug effects Life Sciences & Biomedicine Microbial Sensitivity Tests Molecular Structure Pharmacology & Pharmacy Physical Sciences Science & Technology Structure-Activity Relationship |
Title | Synthesis and evaluation of novel azoles as potent antifungal agents |
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