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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Benzofuroxan Derivatives as Potent Agents against Multidrug-Resistant Mycobacterium tuberculosis

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Author(s):
Fernandes, Guilherme F. S. [1, 2] ; Campos, Debora L. [1] ; Da Silva, Isabel C. [1] ; Prates, Joao L. B. [1, 2] ; Pavan, Aline R. [1, 2] ; Pavan, Fernando R. [1] ; Dos Santos, Jean L. [1, 2]
Total Authors: 7
Affiliation:
[1] Sao Paulo State Univ UNESP, Sch Pharmaceut Sci, Araraquara Jau Highway KM 01, BR-14800903 Araraquara, SP - Brazil
[2] Sao Paulo State Univ UNESP, Inst Chem, Francisco Degni St 55, BR-14800060 Araraquara, SP - Brazil
Total Affiliations: 2
Document type: Journal article
Source: CHEMMEDCHEM; v. 16, n. 8 FEB 2021.
Web of Science Citations: 0
Abstract

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]oxadiaz ole 1-N-oxide (5 b) was particularly remarkable in this regard as it demonstrated MIC90 values below 0.28 mu M 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. (AU)

FAPESP's process: 18/00163-0 - Development and search of new antimicrobials against Tuberculosis: from screening to pre-clinical studies in vivo
Grantee:Fernando Rogério Pavan
Support type: Regular Research Grants
FAPESP's process: 18/17739-2 - Synthesis of New Nitroimidazooxazine Derivatives Designed as Antitubercular Agents
Grantee:Guilherme Felipe dos Santos Fernandes
Support type: Scholarships abroad - Research Internship - Doctorate
FAPESP's process: 18/21778-3 - Analysis of in vitro, in vivo and mechanism of action of benzofuroxan compounds against Mycobacterium tuberculosis
Grantee:Debora Leite Campos
Support type: Scholarships in Brazil - Doctorate
FAPESP's process: 18/24783-8 - Molecular toxicology testing of benzofuraxanes
Grantee:Isabel Cristiane da Silva
Support type: Scholarships abroad - Research Internship - Post-doctor
FAPESP's process: 18/11079-0 - Synthesis and antitubercular activity of new N-oxide compounds designed to treat multiresistant-tuberculosis
Grantee:Jean Leandro dos Santos
Support type: Regular Research Grants
FAPESP's process: 16/09502-7 - Design, synthesis and antitubercular activity of new oxazolidinones useful for the treatment of multidrug-resistant tuberculosis
Grantee:Guilherme Felipe dos Santos Fernandes
Support type: Scholarships in Brazil - Doctorate