Bioorganic & Medicinal Chemistry Letters 2010-07-15

Synthesis and biological activity of 2-hydroxynicotinoyl-serine-butyl esters related to antibiotic UK-3A.

Ade Arsianti, Muhammad Hanafi, Endang Saepudin, Tsumoru Morimoto, Kiyomi Kakiuchi

Index: Bioorg. Med. Chem. Lett. 20(14) , 4018-20, (2010)

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Abstract

Novel 2-hydroxynicotinoyl-serine-butyl esters have been synthesized. Three-step reactions from L-serine by esterification with n-butanol, amidation with 2-hydroxynicotinic acid and esterification with the corresponding carboxylic acids gave AD-1, AD-2 and AD-3. The toxicity level of esters were determined by Brine shrimp assay, and antibiotic activity was tested against Escherichia coli, Bacillus subtilis, Staphylococcus aureus and Candida albicans. AD-3 showed greater activity as a growth inhibitor of B. subtilis and S. aureus compared to Antimycin A(3).2010 Elsevier Ltd. All rights reserved.

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