biostudies-literatureZhao HMinistry of Science and Technology of the People's Republic of ChinaMinistry of Education of the People's Republic of ChinaNational Natural Science Foundation of China533-537https://www.ebi.ac.uk/biostudies/studies/S-EPMC5430409biostudies-literatureUnknown8(5)A novel series of fluorine-containing benzoxazinyl-oxazolidinones were designed and synthesized as antidrug-resistant tuberculosis agents possessing good activity and improved pharmacokinetic profiles. Compound 21 exhibited not only outstanding in vitro activity with a MIC value of 0.25-0.50 μg/mL against drug-susceptible H37Rv strain and two clinically isolated drug-resistant Mycobacterium tuberculosis strains, but also acceptable in vitro ADME/T properties. Moreover, this compound displayed excellent mouse pharmacokinetic profiles with an oral bioavailability of 102% and a longer elimination half-life of 4.22 h, thereby supporting further optimization and development of this promising lead series.ACS medicinal chemistry lettersDiscovery of Fluorine-Containing Benzoxazinyl-oxazolidinones for the Treatment of Multidrug Resistant Tuberculosis.PMC5430409815029172014CX152015ZX09102007-013Li YMa CZhang DSheng LWang BLu YHuang HWang WWang XYuan ZZhao HfalseDiscovery of Fluorine-Containing Benzoxazinyl-oxazolidinones for the Treatment of Multidrug Resistant Tuberculosis.A novel series of fluorine-containing benzoxazinyl-oxazolidinones were designed and synthesized as antidrug-resistant tuberculosis agents possessing good activity and improved pharmacokinetic profiles. Compound 21 exhibited not only outstanding in vitro activity with a MIC value of 0.25-0.50 μg/mL against drug-susceptible H37Rv strain and two clinically isolated drug-resistant Mycobacterium tuberculosis strains, but also acceptable in vitro ADME/T properties. Moreover, this compound displayed excellent mouse pharmacokinetic profiles with an oral bioavailability of 102% and a longer elimination half-life of 4.22 h, thereby supporting further optimization and development of this promising lead series.2017-01-01T00:00:00Z2017 May2025-04-04T09:08:15.417Z2019-03-26T23:36:31ZS-EPMC54304092852310610.1021/acsmedchemlett.7b00068