%0 Journal Article %J Bioorganic & Medicinal Chemistry %D 2011 %T Design, synthesis and biological evaluation of peptidyl-vinylaminophosphonates as novel cysteine protease inhibitors %A Bhattacharya, Asish K. %A Rana, Kalpeshkumar C. %K Cysteine %K Inhibitor design %K Protease inhibitors %K synthesis %K Tsuji-Trost reaction %K Vinylaminophosphonates %X

We report herein, design and synthesis of vinylaminophosphonates, a novel class of compounds as possible cysteine protease inhibitors. The synthesis of vinylaminophosphonates has been accomplished employing Tsuji-Trost reaction as a key step. The synthesized compounds were assayed against papain, a model cysteine protease and some of our synthesized compounds showed IC50 values in the range of 30-54 mu M thereby suggesting that these chemical entities thus could constitute an interesting template for the design of potential novel protease inhibitors. (C) 2011 Elsevier Ltd. All rights reserved.

%B Bioorganic & Medicinal Chemistry %I PERGAMON-ELSEVIER SCIENCE LTD %C THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND %V 19 %P 7129-7135 %8 DEC %G eng %N 23 %3 Foreign %4 3.47 %R 10.1016/j.bmc.2011.09.058