title: A convenient and efficient approach to polyfluorosalicylic acids and their tuberculostatic activity.
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 6.5μg/mL depending on the structure.
authors.affiliation: Postovsky Institute of Organic Synthesis of Ural Branch of Russian Academy of Science, S. Kovalevsloy Str., 22, Ekaterinburg 620990, Russia. Electronic address: schegolkov@ios.uran.ru.
authors.forename: Evgeny V
authors.initials: EV
authors.lastname: Shchegol'kov
authors.affiliation: Postovsky Institute of Organic Synthesis of Ural Branch of Russian Academy of Science, S. Kovalevsloy Str., 22, Ekaterinburg 620990, Russia.
authors.forename: Irina V
authors.initials: IV
authors.lastname: Shchur
authors.affiliation: Postovsky Institute of Organic Synthesis of Ural Branch of Russian Academy of Science, S. Kovalevsloy Str., 22, Ekaterinburg 620990, Russia.
authors.forename: Yanina V
authors.initials: YV
authors.lastname: Burgart
authors.affiliation: Postovsky Institute of Organic Synthesis of Ural Branch of Russian Academy of Science, S. Kovalevsloy Str., 22, Ekaterinburg 620990, Russia.
authors.forename: Victor I
authors.initials: VI
authors.lastname: Saloutin
authors.affiliation: Perm National Research Polytechnic University, Komsomolsky Av., 29, Perm 614990, Russia.
authors.forename: Sergey Yu
authors.initials: SY
authors.lastname: Solodnikov
authors.affiliation: Perm National Research Polytechnic University, Komsomolsky Av., 29, Perm 614990, Russia.
authors.forename: Olga P
authors.initials: OP
authors.lastname: Krasnykh
authors.affiliation: Ural Research Institute of Phthisiopulmonology, 22 Parts'ezda, 50, Ekaterinburg 620039, Russia.
authors.forename: Marionella A
authors.initials: MA
authors.lastname: Kravchenko
mesh_terms: D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D060326:Chemistry Techniques, Synthetic; D004353:Drug Evaluation, Preclinical / Q000379:methods; D005461:Fluorine / Q000737:chemistry; D017616:Magnesium Compounds / Q000737:chemistry; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D020156:Salicylic Acid / Q000737:chemistry
chemical_list: D000995:Antitubercular Agents; D017616:Magnesium Compounds; D005461:Fluorine; D020156:Salicylic Acid
keywords: Anti-mycobacterial activity; Nucleophilic substitution; Polyfluorosalicylic acid; Toxicity; Tuberculosis