4-Aminopyrimidines as novel HIV-1 inhibitors.
A series of 4-aminopyrimidines (1) was identified as novel HIV inhibitors of unknown molecular target. Structural modifications were carried out to establish its SAR and identify the linking site for target identification. A number of analogs were found to possess single digit inhibitory activity for HIV replication. Several analogs with various potential linkers, including a biotinated analog, also exhibited excellent potency, and could serve as tools for the identification of novel anti-HIV targets.
Gadhachanda
Venkat R
VR
Genomics Institute of the Novartis Research Foundation (GNF), 10675 John Jay Hopkins Drive, San Diego, CA 92121, USA.
Wu
Baogen
B
Wang
Zhiwei
Z
Kuhen
Kelli L
KL
Caldwell
Jeremy
J
Zondler
Helmut
H
Walter
Harald
H
Havenhand
Mark
M
He
Yun
Y
D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects*; D011743:Pyrimidines / Q000737:chemistry*; D013329:Structure-Activity Relationship
D019380:Anti-HIV Agents; D011743:Pyrimidines; C034821:4-aminopyrimidine