Notice: Users may be experiencing issues with displaying some pages on stanfordhealthcare.org. We are working closely with our technical teams to resolve the issue as quickly as possible. Thank you for your patience.
 

Learn about the flu shot, COVID-19 vaccine, and our masking policy »

Stanford Health Care

Analogs design, synthesis and biological evaluation of peptidomimetics with potential anti-HCV activity BIOORGANIC & MEDICINAL CHEMISTRY Lasheen, D. S., Ismail, M. A., Abou El Ella, D. A., Ismail, N. S., Eid, S., Vleck, S., Glenn, J. S., Watts, A. G., Abouzid, K. A. 2013; 21 (10): 2742-2755

Abstract

Two series of peptidomimetics were designed, prepared and evaluated for their anti-HCV activity. One series possesses a C-terminal carboxylate functionality. In the other series, the electrophilic vinyl sulfonate moiety was introduced as a novel class of HCV NS3/4A protease inhibitors. In vitro based studies were then performed to evaluate the efficacies of the inhibitors using Human hepatoma cells, with the vinyl sulfonate ester (10) in particular, found to have highly potent anti-HCV activity with an EC(50) = 0.296 µM. Finally, molecular modeling studies were performed through docking of the synthesized compounds in the HCV NS3/4A protease active site to assess their binding modes with the enzyme and gain further insight into their structure-activity relationships.

View details for DOI 10.1016/j.bmc.2013.03.017

View details for Web of Science ID 000318318700011

View details for PubMedID 23583031