Related Experiment Video
Updated: Jul 11, 2026

Rapid Screening of HIV Reverse Transcriptase and Integrase Inhibitors
Published on: April 9, 2014
Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors
John S Wai1, Boyoung Kim, Thorsten E Fisher
1Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. john_wai@merck.com
Abstract:
A series of potent novel dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors was identified. These compounds inhibited the strand transfer process of HIV-1 integrase and viral replication in cells. Compound 6 is active against replication of HIV with a CIC(95) of 0.31 microM and exhibits no shift in potency in the presence of 50% normal human serum. It displays a good pharmacokinetic profile when dosed in rats and no covalent binding with microsomal proteins in both in vitro and in vivo models.
Related Concept Videos
Antiviral Nucleoside Inhibitors
Inhibitors of Virion Maturation and Assembly
Inhibitors of Viral Protein Synthesis
Retrovirus Life Cycles
Inhibitors Of Virion Release
Dipeptidyl Peptidase 4 Inhibitors

