Literature DB >> 28626525

Identification of Better Pharmacokinetic Benzothiazinone Derivatives as New Antitubercular Agents.

Kai Lv1, Xuefu You1, Bin Wang2, Zengquan Wei3, Yun Chai1, Bo Wang1, Apeng Wang1, Guocheng Huang1, Mingliang Liu1, Yu Lu2.   

Abstract

A series of new 8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one(BTZ) derivatives containing a C-2 nitrogen spiro-heterocycle moiety based on the structures of BTZ candidates BTZ043 and PBTZ169 were designed and synthesized as new antitubercular agents. Many of them were found to have excellent in vitro activity (MIC < 0.15 μM) against the drug susceptive Mycobacterium tuberculosis H37Rv strain and two clinically isolated multidrug-resistant strains. Compounds 11l and 11m display acceptable safety, greater aqueous solubility, and better pharmacokinetic profiles than PBTZ169, suggesting their promising potential to be lead compounds for future antitubercular drug discovery.

Entities:  

Keywords:  Antitubercular agents; benzothiazinones; pharmacokinetics; spiro-heterocycles; structure−activity relationships

Year:  2017        PMID： 28626525      PMCID： PMC5467196          DOI： 10.1021/acsmedchemlett.7b00106

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  30 in total

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  11 in total

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