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 inBioorganic & medicinal chemistry letters Vol. 24; no. 1; pp. 192 - 194
Main Authors Li, Liangjing, Ding, Hao, Wang, Baogang, Yu, Shichong, Zou, Yan, Chai, Xiaoyun, Wu, Qiuye
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier 01.01.2014
Subjects
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
Antifungal activity
CASPOFUNGIN
Azole
Synthesis
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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.
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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Issue 1
Keywords Antifungal activity
CASPOFUNGIN
Azole
Synthesis
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Snippet 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...
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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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https://www.ncbi.nlm.nih.gov/pubmed/24332489
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