Discovery of human CCR5 antagonists containing hydantoins for the treatment of HIV-1 infection.
A series of hydantoin derivatives has been discovered as highly potent nonpeptide antagonists for the human CCR5 receptor. The synthesis, SAR, and biological profiles of this class of antagonists are described.
Kim
D
D
Department of Medicinal Chemistry, Merck Research Laboratories, RY 121-240, PO Box 2000, Rahway, NJ 07065, USA. dooseop_kim@merck.com
Wang
L
L
Caldwell
C G
CG
Chen
P
P
Finke
P E
PE
Oates
B
B
MacCoss
M
M
Mills
S G
SG
Malkowitz
L
L
Gould
S L
SL
DeMartino
J A
JA
Springer
M S
MS
Hazuda
D
D
Miller
M
M
Kessler
J
J
Danzeisen
R
R
Carver
G
G
Carella
A
A
Holmes
K
K
Lineberger
J
J
Schleif
W A
WA
Emini
E A
EA
D019380:Anti-HIV Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D065100:CCR5 Receptor Antagonists; D015658:HIV Infections / Q000188:drug therapy*; D015497:HIV-1 / Q000302:isolation & purification; D006801:Humans; D006827:Hydantoins / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*
D019380:Anti-HIV Agents; D065100:CCR5 Receptor Antagonists; D006827:Hydantoins