Design, synthesis, and SAR of a novel pyrazinone series with non-nucleoside HIV-1 reverse transcriptase inhibitory activity.
A series of novel pyrazinones designed as non-nucleoside reverse transcriptase inhibitors (NNRTIs) was synthesized and their anti-HIV structure-activity relationship (SAR) was studied.
Heeres
Jan
J
Center for Molecular Design, Janssen Pharmaceutica, Antwerpsesteenweg 37, B-2350 Vosselaar, Belgium. jheeres@prdbe.jnj.com
de Jonge
Marc R
MR
Koymans
Lucien M H
LM
Daeyaert
Frits F D
FF
Vinkers
Maarten
M
Van Aken
Koen J A
KJ
Arnold
Eddy
E
Das
Kalyan
K
Kilonda
Amuri
A
Hoornaert
Georges J
GJ
Compernolle
Frans
F
Cegla
Marek
M
Azzam
Rasha A
RA
Andries
Koen
K
de Béthune
Marie-Pierre
MP
Azijn
Hilde
H
Pauwels
Rudi
R
Lewi
Paul J
PJ
Janssen
Paul A J
PA
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D054303:HIV Reverse Transcriptase / Q000378:metabolism*; D015497:HIV-1 / Q000187:drug effects / Q000235:genetics; D008958:Models, Molecular; D009154:Mutation; D011719:Pyrazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D019380:Anti-HIV Agents; D011719:Pyrazines; D018894:Reverse Transcriptase Inhibitors; D054303:HIV Reverse Transcriptase