SECONDARY METABOLITES BY CHEMICAL-SCREENING .17. NIGERICINOL DERIVATIVES - SYNTHESIS, BIOLOGICAL-ACTIVITIES, AND MODELING STUDIES

被引：9

作者：

GRABLEY, S

HAMMANN, P

KLEIN, R

SEIBERT, G

WINKLER, I

KROGER, A

DITZEL, F

机构：

[1] HOECHST AG,POSTFACH 800320,W-6230 FRANKFURT,GERMANY

[2] UNIV FRANKFURT,INST MIKROBIOL,W-6000 FRANKFURT,GERMANY

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1992年 / 35卷 / 05期

关键词：

D O I：

10.1021/jm00083a020

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and the biological activity of C-1-reduced nigericin derivatives (nigericinols) are described and discussed. The dichloronigericinol 7 impressively demonstrated that the C-1 carboxylic acid moiety was not required for a distinct activity against bacteria and viruses. Based on the correlation between K+/H+ antiport activities and antibacterial activities it was deduced that the mode of action of the described nigericinols are related to their ionophoric properties. Molecular modeling studies showed that the efficiency of the nigericinols as ionophores correlates, qualitatively, with the probability of forming a cyclic structure, with the exception of 7.

引用

页码：939 / 944

页数：6

共 29 条

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