1334320-24-9Relevant articles and documents
Design and synthesis of a new series of cyclopropylamino-linking diarylpyrimidines as HIV non-nucleoside reverse transcriptase inhibitors
Liu, Yang,Meng, Ge,Zheng, Aqun,Chen, Fener,Chen, Wenxue,Clercq, Erik De,Pannecouque, Christophe,Balzarini, Jan
, p. 334 - 341 (2014/07/22)
A new series of 29 diarylpyrimidine analogues featuring a cyclopropylamino group between the pyrimidine scaffold and the aryl wing have been synthesized. All of the new compounds have been characterized by spectra analysis. The target molecules were evalu
Synthesis and Anti-HIV Activity of Aryl-2-[(4-cyanophenyl)amino]-4-pyrimidinone hydrazones as Potent Non-nucleoside Reverse Transcriptase Inhibitors
Ma, Xiao-Dong,Yang, Shi-Qiong,Gu, Shuang-Xi,He, Qiu-Qin,Chen, Fen-Er,DeClercq, Erik,Balzarini, Jan,Pannecouque, Christophe
scheme or table, p. 2225 - 2232 (2012/04/11)
A series of novel diarylpyrimidines (DAPYs) with a ketone hydrazone substituent on the methylene linker between the pyrimidine nucleus and the aryl moiety at the C-4 position were synthesized, and their antiviral activity against human immunodeficiency virus (HIV)-1 in MT-4 cells was evaluated. Most compounds of this class exhibited excellent activity against wild-type HIV-1, with EC50 values in the range of 1.7-13.2nM. Of these compounds, 2-bromophenyl-2-[(4-cyanophenyl)amino]-4-pyrimidinone hydrazone (9k) displayed the most potent anti-HIV-1 activity (EC50=1.7±0.6nM), with excellent selectivity for infected over uninfected cells (SI=5762). In addition, the 4-methyl phenyl analogue 9d (EC50=2.4±0.2nM, SI=18461) showed broad spectrum HIV inhibitory activity, with EC50 values of 2.4±0.2nM against wild-type HIV-1, 5.3±0.4μM against HIV-1 double-mutated strain RES056 (K103N+Y181C), and 5.5μM against HIV-2 ROD strain. Furthermore, structure-activity relationship (SAR) data and molecular modeling results for these compounds are also discussed. Antiviral agents: A series of new diarylpyrimidine (DAPY) derivatives with a ketone hydrazine substituent on the CH2 linker between the pyrimidine nucleus and the phenyl ring were synthesized, and their anti-HIV activity in MT-4 cells was evaluated. Most compounds of this class exhibited excellent activity against wild-type HIV-1, with EC50 values in the range of 1.7-13.2nM.