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Elsevier, Bioorganic and Medicinal Chemistry Letters, 21(17), p. 5876-5880

DOI: 10.1016/j.bmcl.2007.08.031

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Structure-based design, synthesis, and biological evaluation of peptidomimetic SARS-CoV 3CLpro inhibitors

Journal article published in 2007 by Arun K. Ghosh, Kai Xi, Valerie Grum-Tokars, Xiaoming Xu, Kiira Ratia, Wentao Fu, Katherine V. Houser, Susan C. Baker, Michael E. Johnson ORCID, Andrew D. Mesecar ORCID
This paper is available in a repository.
This paper is available in a repository.

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Abstract

Structure-based design, synthesis, and biological evaluation of a series of peptidomimetic severe acute respiratory syndrome-coronavirus chymotrypsin-like protease inhibitors are described. These inhibitors were designed and synthesized based upon our X-ray crystal structure of inhibitor 1 bound to SARS-CoV 3CLpro. Incorporation of Boc-Ser as the P(4)-ligand resulted in enhanced SARS-CoV 3CLpro inhibitory activity. Structural analysis of the inhibitor-bound X-ray structure revealed high binding affinity toward the enzyme.