期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 18, 期 10, 页码 3618-3624出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.03.033
关键词
Silica-supported fluoroboric acid; Thiomorpholide; Solvent-free conditions; Willgerodt-Kindler reaction; Erwinia carotovora; L-Asparaginase; Antioxidant activity
An efficient solvent-free procedure for the synthesis of thiomorpholides in the presence of a catalytic amount of solid-supported fluoroboric acid (HBF4-SiO2) is described. The advantages of this method are high yields, short reaction times, ease of product isolation, low cost, and the catalyst can be recycled for a number of times without significant loss of activity. Three thiomorpholides possessing electron-donating group (4c, 4g, and 4h) were exhibiting excellent stimulatory activities against Erwinia carotovora L-asparaginase. The most potent activator, compound 4h displayed the following kinetic parameters, K-m = 75 mu M and V-max = 1000 mu mol mg(-1) min(-1) and K-A = 0.985 mu M. Furthermore, these compounds (4g, 4h, 4c, 4f, 4a, and 4d) have also shown promising 2,2'-diphenyl-1-picrylhydrazyl (DPPH) reducing antioxidant activity (21-36%) at 1 mM concentration as compared to standard butylated hydroxyl anisole (72% at 1 mM). (C) 2010 Published by Elsevier Ltd.
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