A convenient and efficient approach to polyfluorosalicylic acids and their tuberculostatic activity. Issue 10 (15th May 2016)

• Record Type: Journal Article
• Authors: Shchegol'kov, Evgeny V.; Shchur, Irina V.; Burgart, Yanina V.; Saloutin, Victor I.; Solodnikov, Sergey Yu.; Krasnykh, Olga P.; Kravchenko, Marionella A.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 10(2016)
• Page Start: 2455
• Page End: 2458
• Publication Date: 2016-05-15
• Subjects: Polyfluorosalicylic acid -- Nucleophilic substitution -- Anti-mycobacterial activity -- Tuberculosis -- Toxicity; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.03.107
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: We have developed the practical method for polyfluorosalicylic acids synthesis via nucleophilic ortho - mono -substitution of fluorine atom with magnesium methoxide. We have managed to increase the yield of targeted polyfluorosalicylic acids from good to quantitative. We have studied the tuberculostatic activity of polyfluorosalicylic acids. It has been found that minimum inhibitory concentration (MIC) of compounds is from 0.7 to 6.5 μg/mL depending on the structure.