☆ 4.4 Article

Synthesis and Antifungal Activity of 1-[(2-Benzyloxy)Phenyl]-2-(Azol-1-yl)Ethanone Derivatives: Exploring the Scaffold Flexibility

CHEMICAL BIOLOGY & DRUG DESIGN (2011)

期刊

CHEMICAL BIOLOGY & DRUG DESIGN

卷 78, 期 6, 页码 979-987

出版社

WILEY-BLACKWELL

DOI: 10.1111/j.1747-0285.2011.01243.x

关键词

1; 2; 4-triazole; 1H-imidazole; antifungal activity; azole antifungals; conformational study

类别

Biochemistry & Molecular Biology Chemistry, Medicinal

资金

Research Council of Mazandaran University of Medical Sciences, Sari, Iran

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Protocol

Reagent

摘要

Based on the N-(phenethyl)azole backbone of azole antifungals, we designed 1-[(2-benzyloxy)phenyl]-2-(azol-1-yl)ethanone derivatives 2 and 3, containing benzyloxyphenyl scaffold of croconazole. Also these compounds can be considered as flexible analogs, resulted from C2C3 disconnection of 3'-chloro-3-imidazolylflavanone 1, recently described as antifungal agent. Thus, in this report, we describe the synthesis of 1-[(2-benzyloxy)phenyl]-2-(azol-1-yl)ethanone derivatives 2 and 3 and their biological evaluation against different pathogenic fungi. By comparing the antifungal activity profile of flexible compounds 2 and 3 with that of rigid analog 1, it can be inferred that lower susceptibilities (higher minimum inhibitory concentrations) were observed with flexible compounds. However, among the synthesized compounds, 1-[2-(2,4-dichlorobenzyloxy)phenyl]-2-(1H-imidazol-1-yl)ethanone hydrochloride (2g) showed comparable or more potent antifungal activity in comparison with fluconazole as a standard drug.

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