A convenient and efficient approach to polyfluorosalicylic acids and their tuberculostatic activity

[Display omitted] 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...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2016-05, Vol.26 (10), p.2455-2458
Hauptverfasser:	Shchegol’kov, Evgeny V., Shchur, Irina V., Burgart, Yanina V., Saloutin, Victor I., Solodnikov, Sergey Yu, Krasnykh, Olga P., Kravchenko, Marionella A.
Format:	Artikel
Sprache:	eng
Schlagworte:	Anti-mycobacterial activity Antitubercular Agents - chemical synthesis Antitubercular Agents - chemistry Antitubercular Agents - pharmacology Chemistry Techniques, Synthetic Drug Evaluation, Preclinical - methods Fluorine - chemistry Magnesium Compounds - chemistry Microbial Sensitivity Tests Molecular Structure Mycobacterium tuberculosis - drug effects Nucleophilic substitution Polyfluorosalicylic acid Salicylic Acid - chemistry Toxicity Tuberculosis
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Zusammenfassung:	[Display omitted] 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 6.5μg/mL depending on the structure.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2016.03.107