Exploiting the furo [2,3-b]pyridine core against multidrug-resistant Mycobacterium tuberculosis

Author(s)

Fumagalli, Fernando ^[1] ; Gil de Melo, Shaiani Maria ^[1] ; Ribeiro, Camila Maringolo ^[2] ; Solcia, Mariana Cristina ^[2] ; Pavan, Fernando Rogerio ^[2] ; Emery, Flavio da Silva ^[2]

Affiliation

^[1] Univ Sao Paulo FCFRP USP, Dept Pharmaceut Sci, Sch Pharmaceut Sci Ribeirao Preto, Av Cafe S-N Campus Univ USP, BR-14040903 Ribeirao Preto, SP - Brazil

^[2] Sao Paulo State Univ UNESP, Dept Biol Sci, Sch Pharmaceut Sci, Rodovia Araraquara Jau Km01 S-N, Campos Ville, BR-14800903 Araraquara - Brazil

• Document type: Journal article
• Source: Bioorganic & Medicinal Chemistry Letters; v. 29, n. 8, p. 974-977, APR 15 2019.
• Web of Science Citations: 0

Abstract

Identification of new antibiotics suitable for the treatment of tuberculosis is required. In addition to selectivity, it is necessary to find new antibiotics that are effective when the tuberculous mycobacteria are resistant to the available therapies. The furo {[}2,3-b]pyridine core offers potential for this application. Herein, we have described the screening of our in-house library of furopyridines against Mycobacterium tuberculosis and identified a promising selective bioactive compound against different drug-resistant strains of this mycobacteria. The library of compounds was prepared by a C-H amination reaction using mild and metal-free conditions, increasing the available information about the reactivity of furo {[}2,3-b] pyridine core through this reaction. (AU)

• FAPESP's process: 14/50265-3 - Distribution and metabolism of natural and synthetic xenobiotics: from the comprehension of reactional process to tissue imaging generation
• Grantee: Norberto Peporine Lopes
• Support Opportunities: BIOTA-FAPESP Program - Thematic Grants
• FAPESP's process: 17/21146-4 - Heterocyclic chemistry and epigenetic for the development of library of compounds for medicinal chemistry purposes.
• Grantee: Flavio da Silva Emery
• Support Opportunities: Regular Research Grants
• FAPESP's process: 15/06588-5 - Development of library of heterocyclic fragments based on new heteroaromatic cores
• Grantee: Fernando Fumagalli
• Support Opportunities: Scholarships in Brazil - Doctorate
• 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 Opportunities: Regular Research Grants