Ma, Xiao-Dong; Yang, Shi-Qiong; Gu, Shuang-Xi; He, Qiu-Qin; Chen, Fen-Er; De Clercq, Erik; Balzarini, Jan; Pannecouque, Christophe published the artcile< Synthesis and Anti-HIV Activity of Aryl-2-[(4-cyanophenyl)amino]-4-pyrimidinone hydrazones as Potent Non-nucleoside Reverse Transcriptase Inhibitors>, Reference of 658-99-1, the main research area is preparation antiviral HIV cyanophenyl amino pyrimidinone hydrazone RT inhibitor.
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 1.7-13.2 nM. Of these compounds, 2-bromophenyl-2-[(4-cyanophenyl)amino]-4-pyrimidinone hydrazone (9 k) displayed the most potent anti-HIV-1 activity (EC50=1.7±0.6 nM), with excellent selectivity for infected over uninfected cells (SI=5762). In addition, the 4-Me Ph analog 9 d (EC50=2.4±0.2 nM, SI=18461) showed broad spectrum HIV inhibitory activity, with EC50 values of 2.4±0.2 nM against wild-type HIV-1, 5.3±0.4 μM against HIV-1 double-mutated strain RES056 (K103N+Y181C), and 5.5 μM against HIV-2 ROD strain. Furthermore, structure-activity relationship (SAR) data and mol. modeling results for these compounds are also discussed.
ChemMedChem published new progress about Antiviral agents. 658-99-1 belongs to class nitriles-buliding-blocks, and the molecular formula is C8H5F2N, Reference of 658-99-1.
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts