Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
The synthesis and anti-HIV-1 activity of a series of diarylpyrimidines (DAPYs) are described. Several members of this novel class of non-nucleoside reverse transcriptase inhibitors (NNRTIs) are extremely potent against both wild-type and a panel of clinically significant single- and double-mutant strains of HIV-1.
Ludovici
D W
DW
Janssen Research Foundation, Welsh and McKean Roads, Spring House, PA 19477, USA.
De Corte
B L
BL
Kukla
M J
MJ
Ye
H
H
Ho
C Y
CY
Lichtenstein
M A
MA
Kavash
R W
RW
Andries
K
K
de Béthune
M P
MP
Azijn
H
H
Pauwels
R
R
Lewi
P J
PJ
Heeres
J
J
Koymans
L M
LM
de Jonge
M R
MR
Van Aken
K J
KJ
Daeyaert
F F
FF
Das
K
K
Arnold
E
E
Janssen
P A
PA
D019380:Anti-HIV Agents / Q000737:chemistry* / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors / Q000187:drug effects / Q000235:genetics; D015497:HIV-1 / Q000187:drug effects / Q000235:genetics; D020128:Inhibitory Concentration 50; D009154:Mutation; D009570:Nitriles / Q000737:chemistry* / Q000494:pharmacology*; D011743:Pyrimidines / Q000737:chemistry* / Q000494:pharmacology*; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
C442363:6-amino-5-bromo-4-(4-cyano-2,6-dimethylphenoxy)-2-(4-cyanophenylamino)pyrimidine; D019380:Anti-HIV Agents; D009570:Nitriles; D011743:Pyrimidines; D018894:Reverse Transcriptase Inhibitors; D054303:HIV Reverse Transcriptase