Article
First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain.
Bioorganic & medicinal chemistry letters - 1 May 2018
Huang Boshi, Liu Xinhao, Tian Ye, Kang Dongwei, Zhou Zhongxia, Daelemans Dirk, De Clercq Erik, Pannecouque Christophe, Zhan Peng, Liu Xinyong
Abstract excerpt
In the present work, we described the synthesis, antiviral profiles and metabolic stability in human plasma of compound 6, a potential carbonate prodrug of HIV-1 NNRTI drug candidate RDEA427. Compound 6 was found to inhibit the wild-type (WT) and K103N/Y181C double mutant HIV-1 strains at nano- and submicromolar concentrations, respectively. Moreover, it displayed potent HIV-1 reverse transcriptase inhibitory...
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.
