BIP! Finder - Development of potent dipeptide-type SARS-CoV 3CL protease inhibitors with novel P3 scaffolds: Design, synthesis, biological evaluation, and docking studies

2013 • Development of potent dipeptide-type SARS-CoV 3CL protease inhibitors with novel P3 scaffolds: Design, synthesis, biological evaluation, and docking studies

Authors: Ernesto Freire; Takehito Yamamoto; Shen En Chen; Aurash Naser-Tavakolian; Kentaro Takayama; Yuji Koiwai; Arne Schön; Sho Konno; Kenichi Akaji; Fumika Yakushiji; Akihiro Taguchi; Pillaiyar Thanigaimalai; Yoshio Hayashi

Venue: European Journal of Medicinal Chemistry

Type: Publication

Abstract: We report the design and synthesis of a series of dipeptide-type inhibitors with novel P3 scaffolds that display potent inhibitory activity against SARS-CoV 3CLpro. A docking study involving binding between the dipeptidic lead compound 4 and 3CLpro suggested the modification of a structurally flexible P3 N-(3-methoxyphenyl)glycine with various rigid P3 moieties in 4. The modifications led to the identification of several potent derivatives, including 5c-k and 5n with the inhibitory activities (Ki or IC50) in the submicromolar to nanomolar range... (read more)

Impact:

6.515072E-8 6.0246177E-9 74 1

/ Attention: 0 15

Topics: Stereochemistry Combinatorial chemistry

DOI: 10.1016/j.ejmech.2013.07.037

External links: Crossref OpenAIRE

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