Author(s): Fernandes, Guilherme F. S. [UNESP] ; Campos, Débora L. [UNESP] ; Da Silva, Isabel C. [UNESP] ; Prates, João L. B. [UNESP] ; Pavan, Aline R. [UNESP] ; Pavan, Fernando R. [UNESP] ; Dos Santos, Jean L. [UNESP]
Date: 2021
Persistent ID: http://hdl.handle.net/11449/208395
Origin: Oasisbr
Subject(s): antitubercular agents; benzofuroxan; multidrug-resistant TB; N-oxide; tuberculosis
Made available in DSpace on 2021-06-25T11:11:25Z (GMT). No. of bitstreams: 0 Previous issue date: 2021-04-20
Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
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.
School of Pharmaceutical Sciences São Paulo State University (UNESP), Araraquara Jaú Highway KM 01
Institute of Chemistry São Paulo State University (UNESP), Francisco Degni Street 55
School of Pharmaceutical Sciences São Paulo State University (UNESP), Araraquara Jaú Highway KM 01
Institute of Chemistry São Paulo State University (UNESP), Francisco Degni Street 55
FAPESP: 2016/09502-7
FAPESP: 2018/00163-0
FAPESP: 2018/11079-0
FAPESP: 2018/17739-2
FAPESP: 2018/21778-3
FAPESP: 2018/24783-8
CNPq: 404181/2019-8
CNPq: 429139/2018-7
