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Design and synthesis of dipeptidyl glutaminyl fluoromethyl ketones as potent severe acute respiratory syndrome coronovirus (SARS-CoV) inhibitors.

Zhang, Han-Zhong, Zhang, Hong, Kemnitzer, William, Tseng, Ben, Cinatl, Jindrich, Michaelis, Martin, Doerr, Hans Wilhelm, Cai, Sui Xiong (2006) Design and synthesis of dipeptidyl glutaminyl fluoromethyl ketones as potent severe acute respiratory syndrome coronovirus (SARS-CoV) inhibitors. Journal of Medicinal Chemistry, 49 (3). pp. 1198-201. ISSN 0022-2623. (doi:10.1021/jm0507678) (The full text of this publication is not currently available from this repository. You may be able to access a copy if URLs are provided) (KAR id:34100)

The full text of this publication is not currently available from this repository. You may be able to access a copy if URLs are provided.
Official URL:
https://doi.org/10.1021/jm0507678

Abstract

This paper describes the design and synthesis of dipeptidyl N,N-dimethyl glutaminyl fluoromethyl ketones (fmk) as severe acute respiratory syndrome coronovirus (SARS-CoV) inhibitors. The compounds were tested against SARS-CoV-induced cell death in Vero or CaCo2 cells as a measurement of the inhibiting effects of the compounds on the replication of the virus. Z-Leu-Gln(NMe(2))-fmk (6a) was found to be a potent inhibitor with low toxicity in cells, protecting cells with an EC(50) value of 2.5 microM and exhibiting a selectivity index of >40.

Item Type: Article
DOI/Identification number: 10.1021/jm0507678
Subjects: R Medicine > RM Therapeutics. Pharmacology
Divisions: Divisions > Division of Natural Sciences > Biosciences
Depositing User: Martin Michaelis
Date Deposited: 05 Jun 2013 20:52 UTC
Last Modified: 09 Mar 2023 11:32 UTC
Resource URI: https://kar.kent.ac.uk/id/eprint/34100 (The current URI for this page, for reference purposes)

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