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New developments for the design,synthesis and biological evaluation of potent SARS-CoV 3CLpro inhibitors
Authors:Thomas Regnier  Diganta Sarma  Koushi Hidaka  Usman Bacha  Ernesto Freire  Yoshio Hayashi  Yoshiaki Kiso
Affiliation:1. Department of Medicinal Chemistry, Center for Frontier Research in Medicinal Science, 21st Century COE Program, Kyoto Pharmaceutical University, Kyoto 607-8412, Japan;2. Department of Biology, Johns Hopkins University, Baltimore, MD, USA;3. Department of Medicinal Chemistry, School of Pharmacy, Tokyo University of Pharmacy and Life Sciences, Tokyo 192-0392, Japan
Abstract:A series of trifluoromethyl, benzothiazolyl or thiazolyl ketone-containing peptidic compounds as SARS-CoV 3CL protease inhibitors were developed and their potency was evaluated by in vitro protease inhibitory assays. Three candidates had encouraging results for the development of new anti-SARS compounds.
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