Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1

Baogen Wu; Kelli Kuhen; Truc Ngoc Nguyen; David Ellis; Beth Anaclerio; Xiaohui He; Kunyong Yang; Donald Karanewsky; Hong Yin; Karen Wolff; Kimberly Bieza; Jeremy Caldwell; Yun He

doi:10.1016/j.bmcl.2006.04.012

Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1

Bioorg Med Chem Lett. 2006 Jul 1;16(13):3430-3. doi: 10.1016/j.bmcl.2006.04.012. Epub 2006 Apr 24.

Authors

Baogen Wu¹, Kelli Kuhen, Truc Ngoc Nguyen, David Ellis, Beth Anaclerio, Xiaohui He, Kunyong Yang, Donald Karanewsky, Hong Yin, Karen Wolff, Kimberly Bieza, Jeremy Caldwell, Yun He

Affiliation

¹ Genomics Institute of the Novartis Research Foundation, GNF, 10675 John Jay Hopkins Dr. San Diego, CA 92121, USA. bwu@gnf.org

PMID: 16632349
DOI: 10.1016/j.bmcl.2006.04.012

Abstract

The synthesis and preliminary structure-activity relationship of a series of pyrrolidinones are described. These pyrrolidinones have been characterized as novel non-nucleoside reverse transcriptase inhibitors (NNRTIs) which are highly potent against wild-type and drug-resistant human immunodeficiency viruses (HIV-1).

MeSH terms

Anti-HIV Agents / chemical synthesis*
Anti-HIV Agents / chemistry
Anti-HIV Agents / pharmacology*
HIV Reverse Transcriptase / antagonists & inhibitors
HIV-1 / drug effects*
Humans
Microbial Sensitivity Tests
Molecular Structure
Pyrrolidinones / chemical synthesis*
Pyrrolidinones / chemistry
Pyrrolidinones / pharmacology*
Reverse Transcriptase Inhibitors / chemical synthesis*
Reverse Transcriptase Inhibitors / chemistry
Reverse Transcriptase Inhibitors / pharmacology*
Structure-Activity Relationship
Virus Replication / drug effects

Substances

Anti-HIV Agents
Pyrrolidinones
Reverse Transcriptase Inhibitors
HIV Reverse Transcriptase