Cyclophilins are host cellular factors which have enzymatic cis-trans Peptidyl-Prolyl Isomerase activity (PPIase). The cyclophilin family of enzymes has 17 human isoforms. Among these, cyclophilin A is the most abundant form and is the best studied. Cyclophilin A has been shown to bind to Cyclosporine (PDB ID: 1CWB  ), this complex recruits calcineurin, which ultimately leads to immunosuppressive activity. It has been further demonstrated that cyclophilin A inhibition without calcineurin recruitment can result in anti-HIV and anti-HCV activity in cell culture. Using X-ray crystal structures and docking studies, we have designed a series of novel compounds represented by 1  for analysis of cyclophilin A inhibition. This presentation will include the design, synthesis and biological activity of selected compounds.                                                            

Cyclophilin A inhibitors as potential anti-HIV agents

246th National Meeting (2013)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.