Design, synthesis and biological evaluation of a library of thiocarbazates and their activity as cysteine protease inhibitors

…, PA Benedetti, SL Diamond, B Smith III…

Index: Liu, Zhuqing; Myers, Michael C.; Shah, Parag P.; Beavers, Mary Pat; Benedetti, Phillip A.; Diamond, Scott L.; Smith, Amos B.; Huryn, Donna M. Combinatorial Chemistry and High Throughput Screening, 2010 , vol. 13, # 4 p. 337 - 351

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Citation Number: 5

Abstract

Recently, we identified a novel class of potent cathepsin L inhibitors, characterized by a thiocarbazate warhead. Given the potential of these compounds to inhibit other cysteine proteases, we designed and synthesized a library of thiocarbazates containing diversity elements at three positions. Biological characterization of this library for activity against a panel of proteases indicated a significant preference for members of the papain family of ...