New developments for the design, synthesis and biological evaluation of potent SARS-CoV 3CL(pro) inhibitors.
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.
Department of Medicinal Chemistry, Center for Frontier Research in Medicinal Science, Kyoto Pharmaceutical University, Japan.
Thomas
T
Regnier
Diganta
D
Sarma
Koushi
K
Hidaka
Usman
U
Bacha
Ernesto
E
Freire
Yoshio
Y
Hayashi
Yoshiaki
Y
Kiso
D000595:Amino Acid Sequence; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D052160:Benzothiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D053818:Chymases / Q000037:antagonists & inhibitors / Q000378:metabolism; D003198:Computer Simulation; D000086782:Coronavirus 3C Proteases; D003546:Cysteine Endopeptidases / Q000378:metabolism; D015195:Drug Design; D007659:Ketones / Q000138:chemical synthesis / Q000737:chemistry; D010455:Peptides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011760:Pyrrolidinones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D045473:Severe acute respiratory syndrome-related coronavirus; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D014764:Viral Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism
D000998:Antiviral Agents; D052160:Benzothiazoles; D007659:Ketones; D010455:Peptides; D011480:Protease Inhibitors; D011760:Pyrrolidinones; D013844:Thiazoles; D014764:Viral Proteins; D053818:Chymases; D003546:Cysteine Endopeptidases; D000086782:Coronavirus 3C Proteases