Bioorganic & medicinal chemistry

Synthesis and preliminary antibacterial evaluation of simplified thiomarinol analogs

O Marion, X Gao, S Marcus, DG Hall

Index: Marion, Olivier; Gao, Xuri; Marcus, Sandra; Hall, Dennis G. Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 3 p. 1006 - 1017

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Citation Number: 8

Abstract

A series of simplified thiomarinol derivatives was prepared by way of catalytic enantioselective inverse electron demand hetero [4+ 2] cycloaddition/allylboration tandem reaction. As a preliminary evaluation, these analogs were tested for antimicrobial activity using a standard disk diffusion assay. Whereas amide analogs were less active, the simple ester analogs 3 and 4 were demonstrated to be more active than thiomarinol H.