Benzofuroxan Derivatives as Potent Agents against Multidrug-Resistant Mycobacterium tuberculosis.
Guilherme Felipe Dos Santos FernandesDébora L CamposIsabel C Da SilvaJoão L B PratesAline R PavanFernando R PavanJean L Dos SantosPublished in: ChemMedChem (2021)
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.
Keyphrases
- multidrug resistant
- mycobacterium tuberculosis
- drug resistant
- acinetobacter baumannii
- gram negative
- pulmonary tuberculosis
- escherichia coli
- klebsiella pneumoniae
- infectious diseases
- healthcare
- public health
- mental health
- positron emission tomography
- computed tomography
- hiv aids
- social media
- hepatitis c virus
- quality improvement
- pet ct
- health promotion
- drug induced