{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Zhao H"],"funding":["Ministry of Science and Technology of the People's Republic of China","Ministry of Education of the People's Republic of China","National Natural Science Foundation of China"],"pagination":["533-537"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC5430409"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["8(5)"],"pubmed_abstract":["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."],"journal":["ACS medicinal chemistry letters"],"pubmed_title":["Discovery of Fluorine-Containing Benzoxazinyl-oxazolidinones for the Treatment of Multidrug Resistant Tuberculosis."],"pmcid":["PMC5430409"],"funding_grant_id":["81502917","2014CX15","2015ZX09102007-013"],"pubmed_authors":["Li Y","Ma C","Zhang D","Sheng L","Wang B","Lu Y","Huang H","Wang W","Wang X","Yuan Z","Zhao H"],"additional_accession":[]},"is_claimable":false,"name":"Discovery of Fluorine-Containing Benzoxazinyl-oxazolidinones for the Treatment of Multidrug Resistant Tuberculosis.","description":"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.","dates":{"release":"2017-01-01T00:00:00Z","publication":"2017 May","modification":"2025-04-04T09:08:15.417Z","creation":"2019-03-26T23:36:31Z"},"accession":"S-EPMC5430409","cross_references":{"pubmed":["28523106"],"doi":["10.1021/acsmedchemlett.7b00068"]}}