Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
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).
Wu
Baogen
B
Genomics Institute of the Novartis Research Foundation, GNF, 10675 John Jay Hopkins Dr. San Diego, CA 92121, USA. bwu@gnf.org
Kuhen
Kelli
K
Ngoc Nguyen
Truc
T
Ellis
David
D
Anaclerio
Beth
B
He
Xiaohui
X
Yang
Kunyong
K
Karanewsky
Donald
D
Yin
Hong
H
Wolff
Karen
K
Bieza
Kimberly
K
Caldwell
Jeremy
J
He
Yun
Y
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011760:Pyrrolidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014779:Virus Replication / Q000187:drug effects
D019380:Anti-HIV Agents; D011760:Pyrrolidinones; D018894:Reverse Transcriptase Inhibitors; D054303:HIV Reverse Transcriptase