Synthesis and antifungal activities of myristic acid analogs

被引：58

作者：

Parang, K ^{[1
]}

Knaus, EE ^{[1
]}

Wiebe, LI ^{[1
]}

Sardari, S ^{[1
]}

Daneshtalab, M ^{[1
]}

Csizmadia, F ^{[1
]}

机构：

[1] UNIV TORONTO,DEPT PHARMACOL,TORONTO,ON M5S 1A8,CANADA

来源：

ARCHIV DER PHARMAZIE | 1996年 / 329卷 / 11期

关键词：

myristic acid; antifungal activity; myristoyl CoA:protein N-myristoyltransferase (NMT); structure-activity relationships;

D O I：

10.1002/ardp.19963291102

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Myristic acid analogs that are putative inhibitors of N-myristoyltransferase were tested in vitro for activity against yeasts (Saccharomyces cerevisiae, Candida albicans, Cryptococcus neoformans) and filamentous fungi (Aspergillus niger). Several (+/-)-2-halotetradecanoic acids including (+/-)-2-bromotetradecanoic acid (14c) exhibited potent activity against C. albicans (MIG = 39 mu M), C. neoformans (MIC = 20 mu M), S. cerevisiae (MIC = 10 mu M), and A. niger (MIC < 42 mu M) in RPMI 1640 media. Improved synthetic methods have been developed for the synthesis of 12-fluorododecanoic acid (12a) and 12-chlorododecanoic acid (12c). Three novel fatty acids, 12-chloro-4-oxadodecanoic acid (8a), 12-phenoxydodecanoic acid (12i), and 11-(4-iodophenoxy)-undecanoic acid (13d) were also synthesized and tested.

引用

页码：475 / 482

页数：8

共 28 条

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