Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles
Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles
复制标题
DOI：
10.1021/acs.jmedchem.9b01446
复制
发表时间：
2019-12-26
影响因子：
7.3
通讯作者：
Chen, Fener
中科院分区：
文献类型：
--
作者：
Sang, Yali;Han, Sheng;Chen, Fener
开发了一系列非二甲基苯基二芳基嘧啶类化合物，其细胞毒性远低于它们的二甲基类似物。含有二氟联苯部分的化合物B13对WT、突变株和RT显示出最高的抗病毒活性。与ETR相比，B13盐酸盐的水溶性提高了5.6微克/毫升(
A series of nondimethylphenyl-diarylpyrimidines with much lower cytotoxicities than their dimethyl analogues were developed. Compound B13 with a difluorobiphenyl moiety showed the highest antiviral activity against WT, mutant strains, and RT. The hydrochloride form of B13 exhibited an improved water solubility of 5.6 mu g/mL compared with ETR (