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Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.

Abstract：

: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 μg/mL compared with ETR (≪1 μg/mL), better stability in human and rat liver microsomes, and a great oral bioavailability of 44%, making it promising as a drug candidate. In addition, no apparent toxicity was observed in the acute toxicity assay (2 g/kg) and HE staining.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Sang Y,Han S,Pannecouque C,De Clercq E,Zhuang C,Chen F

doi

10.1021/acs.jmedchem.9b01446

subject

Has Abstract

pub_date

2019-12-26 00:00:00

pages

11430-11436

issue

24

eissn

0022-2623

issn

1520-4804

journal_volume

62

pub_type

杂志文章

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