RETRACTED: Proton-pumping-ATPase-targeted antifungal activity of cinnamaldehyde based sulfonyl tetrazoles (Retracted article. See vol. 57, pg. 483, 2012)

被引：5

作者：

Shreaz, Sheikh ^{[1
]}

Wani, Mohmmad Younus ^{[2
]}

Ahmad, Sheikh Rayees ^{[4
]}

Ahmad, Sheikh Imran ^{[3
]}

Bhatia, Rimple ^{[1
]}

Athar, Fareeda ^{[2
]}

Nikhat, Manzoor ^{[1
]}

Khan, Luqman A. ^{[1
]}

机构：

[1] Jamia Millia Islamia, Enzyme Kinet Lab, Dept Biosci, New Delhi 110025, India

[2] Jamia Millia Islamia, Ctr Interdisciplinary Res Basic Sci, New Delhi 110025, India

[3] Jamia Millia Islamia, Dept Appl Sci & Humanities, New Delhi 110025, India

[4] Indian Inst Technol, Dept Chem, New Delhi 110016, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 48卷

关键词：

Antifungal activity; Candida; Cinnamaldehyde; Tetrazole; Plasma membrane H+-ATPase; MEDIATED FUNGICIDAL ACTIVITY; CANDIDA-ALBICANS; RESISTANCE; SUSCEPTIBILITY; ECHINOCANDIN; MICROSCOPY;

D O I：

10.1016/j.ejmech.2011.12.007

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Azoles are generally fungistatic, and resistance to fluconazole is emerging in several fungal pathogens. We designed a series of cinnamaldehyde based sulfonyl tetrazole derivatives. To further explore the antifungal activity, in vitro studies were conducted against 60 clinical isolates and 6 standard laboratory strains of Candida. The rapid irreversible action of these compounds on fungal cells suggested a membrane-located target for their action. Results obtained indicate plasma membrane H+-ATPase as site of action of the synthesized compounds. Inhibition of H+-ATPase leads to intracellular acidification and cell death. Presence of chloro and nitro groups on the sulfonyl pendant has been demonstrated to be a key structural element of antifungal potency. SEM micrographs of treated Candida cells showed severe cell breakage and alterations in morphology. (C) 2011 Elsevier Masson SAS. All rights reserved.

引用

页码：363 / 370

页数：8

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