Exploiting the furo[2, 3-b]pyridine core against multidrug-resistant Mycobacterium tuberculosis. Issue 8 (15th April 2019)

• Record Type: Journal Article
• Authors: Fumagalli, Fernando; de Melo, Shaiani Maria Gil; Ribeiro, Camila Maríngolo; Solcia, Mariana Cristina; Pavan, Fernando Rogério; da Silva Emery, Flavio
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 29:Issue 8(2019)
• Page Start: 974
• Page End: 977
• Publication Date: 2019-04-15
• Subjects: Furopyridine -- CH activation -- Tuberculosis -- Multidrug-resistant -- Antibiotic; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2019.02.019
• Languages: English
• ISSNs: 0960-894X

Abstract

Fical abstract: Highlights: Development of a library of C-4, C-5 or C-6 functionalized furo[2, 3- b ]pyridines. Furopyridine core expanded the medicinal chemical space of antituberculosis agents. 5aα had the lowest MIC90 against several Mycobacterium tuberculosis (MTB) strains. 5aα was active against the Multidrug-Resistant clinical isolates of MTB. 5aα had good SI and reveals as Hit fragment for further drug discovery programs. 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 CH 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.