Evolution of anti-HIV drug candidates. Part 2: Diaryltriazine (DATA) analogues.
A synthesis program directed toward improving the stability of imidoyl thiourea based non-nucleoside reverse transcriptase inhibitors (NNRTIs) led to the discovery of diaryltriazines (DATAs), a new class of potent NNRTIs. The synthesis and anti-HIV structure-activity relationship (SAR) studies of a series of DATA derivatives are described.
Ludovici
D W
DW
Janssen Research Foundation, Welsh and McKean Roads, Spring House, PA 19477, USA.
Kavash
R W
RW
Kukla
M J
MJ
Ho
C Y
CY
Ye
H
H
De Corte
B L
BL
Andries
K
K
de Béthune
M P
MP
Azijn
H
H
Pauwels
R
R
Moereels
H E
HE
Heeres
J
J
Koymans
L M
LM
de Jonge
M R
MR
Van Aken
K J
KJ
Daeyaert
F F
FF
Lewi
P J
PJ
Das
K
K
Arnold
E
E
Janssen
P A
PA
D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015195:Drug Design; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors* / Q000235:genetics; D015497:HIV-1 / Q000187:drug effects / Q000235:genetics; D020128:Inhibitory Concentration 50; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014227:Triazines / Q000737:chemistry
D019380:Anti-HIV Agents; D018894:Reverse Transcriptase Inhibitors; D014227:Triazines; D054303:HIV Reverse Transcriptase