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

• Published in: Bioorganic & medicinal chemistry letters Vol. 16; no. 13; pp. 3430 - 3433
• Main Authors: Wu, Baogen, Kuhen, Kelli, Ngoc Nguyen, Truc, Ellis, David, Anaclerio, Beth, He, Xiaohui, Yang, Kunyong, Karanewsky, Donald, Yin, Hong, Wolff, Karen, Bieza, Kimberly, Caldwell, Jeremy, He, Yun
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 01.07.2006; Elsevier
• Subjects: Anti-HIV Agents - chemical synthesis; Anti-HIV Agents - chemistry; Anti-HIV Agents - pharmacology; Antibiotics. Antiinfectious agents. Antiparasitic agents; Antiviral; Antiviral agents; Biological and medical sciences; HIV; HIV Reverse Transcriptase - antagonists & inhibitors; HIV-1 - drug effects; Human immunodeficiency virus; Human immunodeficiency virus 1; Humans; Medical sciences; Microbial Sensitivity Tests; Molecular Structure; NNRTI; Pharmacology. Drug treatments; Pyrrolidinone; 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; NNRTI; Antiviral; HIV; Pyrrolidinone; Human; RNA-directed DNA polymerase; HIV-1 virus; Enzyme; Transferases; Non nucleoside compound; Lactam; Retroviridae; Enzyme inhibitor; Lentivirus; In vitro; Pyrrolidine derivatives; Virus; Resistance; Nucleotidyltransferases; Structure activity relation; Reverse transcriptase inhibitor; Human immunodeficiency virus; Pyrrolidone derivatives; Chemical synthesis
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2006.04.012

N-Aryl pyrrolidinones as novel anti-HIV-1 agents is reported. 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).