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某些新型 1-[(3-取代-3-苯基)丙基]-1H-咪唑的合成及抗假丝酵母活性。

Synthesis and anti-candida potential of certain novel 1-[(3-Substituted-3-phenyl)propyl]-1H-imidazoles.

机构信息

Medicinal and Pharmaceutical Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Centre, Giza, Egypt.

出版信息

Arch Pharm (Weinheim). 2011 Dec;344(12):794-801. doi: 10.1002/ardp.201000224. Epub 2011 Oct 11.

DOI:10.1002/ardp.201000224
PMID:21987482
Abstract

The synthesis and anti-Candida activity of 1-[(3-aroyloxy-3-phenyl)propyl]-1H-imidazoles 5a-f and 1-[(3-alkyl/aralkyl/phenyl-3-phenyl)propan-3-ol]-1H-imidazoles 5g-j are reported. The influence of the ester formation and different substitutions on the anti-Candida activity of the alcohol 4 was investigated. Among the newly developed bioactive chemical entities, compounds 5b and 5c displayed minimum inhibitory concentrations (MICs) against Candida albicans and Candida pseudotropicales comparable to that of tioconazole and more potent than miconazole.

摘要

报告了 1-[(3-芳氧基-3-苯基)丙基]-1H-咪唑 5a-f 和 1-[(3-烷基/芳烷基/苯基-3-苯基)丙-3-醇]-1H-咪唑 5g-j 的合成及抗假丝酵母活性。研究了酯化反应和不同取代基对醇 4 的抗假丝酵母活性的影响。在所开发的新型生物活性化学实体中，化合物 5b 和 5c 对白色假丝酵母和热带假丝酵母的最小抑菌浓度（MIC）与噻康唑相当，比咪康唑更有效。

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