Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 62, Issue 24, Pages 11430-11436Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.9b01446
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Funding
- National Natural Science Foundation of P. R China [81872791, 21372050]
- Shanghai Municipal Natural Science Foundation [13ZR1402200]
- Young Elite Scientists Sponsorship Program by the China Association for Science and Technology [2017QNRC061]
- Key Research and Development Program of Ningxia [2019BFG02017, 2018BFH02001]
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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 (<< 1 mu g/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.
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