23450-37-5Relevant articles and documents
Synthesis of 6-naphthoxy and 6-(α-cyanobenzyl)-3, 4-dihydropyrimidin-4-(3 H)-ones as potent HIV-1 inhibitors
Chen, Guo-Shen,Du, Fen,Zhao, Tian-Sheng,Xiong, Yuan-Zhen
, p. 255 - 260 (2018/09/14)
A series of novel dihydroalkoxybenzyloxopyrimidines (S-DABOs) derivatives were synthesized as potent inhibitors of human immunodeficiency virus type-1 (HIV-1) through one-pot procedure. The chemical modification, which included the replacement of the 6-ar
Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: Synthesis, biological investigation and molecular modeling studies
Wu, Hai-Qiu,Yan, Zi-Hong,Chen, Wen-Xue,He, Qiu-Qin,Chen, Fen-Er,De Clercq, Erik,Balzarini, Jan,Daelemans, Dirk,Pannecouque, Christophe
, p. 6477 - 6483 (2013/10/22)
A series of C6-rigid S-DABO analogs characterized by a substituted benzoyl group at C6 position of the pyrimidine ring has been synthesized and biological evaluation as NNRTIs against wild-type HIV-1 strain IIIB, double RT mutant (K103N + Y181C) strain RES056 as well as HIV-2 strain ROD in MT-4 cell cultures. Most of the compounds exhibited moderate antiviral activities. Among them, compound 7q displayed the highest anti-HIV-1 activity with an EC50 value of 0.26 μM and a selectivity index (SI) of 541. The preliminary structure-activity relationship (SAR) of these new S-DABOs was investigated, the target RT was confirmed and docking study was performed.
