Novel indole-3-sulfonamides as potent HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs).
This Letter describes the design, synthesis, and biological evaluation of novel 3-indole sulfonamides as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) with balanced profiles against common HIV RT mutants K103N and Y181C.
Zhao
Zhijian
Z
Department of Medicinal Chemistry, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA. zhijian_zhao@merck.com
Wolkenberg
Scott E
SE
Sanderson
Philip E J
PE
Lu
Meiqing
M
Munshi
Vandna
V
Moyer
Gregory
G
Feng
Meizhen
M
Carella
Anthony V
AV
Ecto
Linda T
LT
Gabryelski
Lori J
LJ
Lai
Ming-Tain
MT
Prasad
Sridar G
SG
Yan
Youwei
Y
McGaughey
Georgia B
GB
Miller
Michael D
MD
Lindsley
Craig W
CW
Hartman
George D
GD
Vacca
Joseph P
JP
Williams
Theresa M
TM
D018360:Crystallography, X-Ray; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors / Q000235:genetics; D007211:Indoles / Q000737:chemistry*; D008958:Models, Molecular; D009154:Mutation; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology*
D007211:Indoles; D018894:Reverse Transcriptase Inhibitors; D013449:Sulfonamides; C514824:reverse transcriptase, Human immunodeficiency virus 1; D054303:HIV Reverse Transcriptase