Design, synthesis and antitubercular evaluation of benzothiazinones containing an oximido or amino nitrogen heterocycle moiety?
RSC Advances Pub Date: 2017-01-05 DOI: 10.1039/C6RA25712G
Abstract
A series of 8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-ones (BTZs) bearing an oximido or amino nitrogen heterocycle moiety through modifications at the C-2 position of BTZ043 and BPTZ169 were designed and synthesized as new antitubercular agents. Many of the target compounds demonstrate excellent in vitro activity (MIC: <0.016–0.088 μg mL?1) against the drug susceptive H37Rv strain and two clinically isolated multidrug-resistant Mycobacterium tuberculosis (MTB) strains. Compound 10a displays acceptable safety, aqueous solubility and pharmacokinetic properties, opening up a new possibility for further development.
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Journal Name：RSC Advances
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CAS no.: 89640-58-4
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