肺结核
结核分枝杆菌
药品
效力
多重耐药
化学
药理学
医学
抗药性
微生物学
体外
生物
生物化学
病理
作者
Guilherme Fernandes,Denise Campos,Isabel Cristiane da Silva,João Lucas Bruno Prates,Aline Renata Pavan,Fernando Rogério Pavan,Jean Leandro dos Santos
出处
期刊:ChemMedChem
[Wiley]
日期:2021-02-09
卷期号:16 (8): 1268-1282
被引量:9
标识
DOI:10.1002/cmdc.202000899
摘要
Tuberculosis (TB) is currently the leading cause of death related to infectious diseases worldwide, as reported by the World Health Organization. Moreover, the increasing number of multidrug-resistant tuberculosis (MDR-TB) cases has alarmed health agencies, warranting extensive efforts to discover novel drugs that are effective and also safe. In this study, 23 new compounds were synthesized and evaluated in vitro against the drug-resistant strains of M. tuberculosis. The compound 6-((3-fluoro-4-thiomorpholinophenyl)carbamoyl)benzo[c][1,2,5]oxadiazole 1-N-oxide (5 b) was particularly remarkable in this regard as it demonstrated MIC90 values below 0.28 μM against all the MDR strains evaluated, thus suggesting that this compound might have a different mechanism of action. Benzofuroxans are an attractive new class of anti-TB agents, exemplified by compound 5 b, with excellent potency against the replicating and drug-resistant strains of M. tuberculosis.
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