A convenient and efficient approach to polyfluorosalicylic acids and their tuberculostatic activity / Shchegol'kov Evgeny V.,Shchur Irina V.,Burgart Yanina V.,Saloutin Victor I.,Solodnikov Sergey Yu.,Krasnykh Olga P.,Kravchenko Marionella A. // BIOORGANIC \& MEDICINAL CHEMISTRY LETTERS. - 2016. - V. 26, l. 10. - P. 2455-2458.

ISSN/EISSN:

0960-894X / 1464-3405

Type:

Article

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 mu g/mL depending on the structure. (C) 2016 Elsevier Ltd. All rights reserved.

Author keywords:

Polyfluorosalicylic acid; Nucleophilic substitution; Anti-mycobacterial activity; Tuberculosis; Toxicity MYCOBACTERIUM-TUBERCULOSIS; PENTAFLUOROBENZOIC ACID; MEDICINAL CHEMISTRY; FLUORINE

DOI:

10.1016/j.bmcl.2016.03.107

Web of Science ID:

ISI:000374217100014

Соавторы в МНС:

Другие поля

Поле	Значение
Month	MAY 15
Publisher	PERGAMON-ELSEVIER SCIENCE LTD
Address	THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND
Language	English
EISSN	1464-3405
Keywords-Plus	MYCOBACTERIUM-TUBERCULOSIS; PENTAFLUOROBENZOIC ACID; MEDICINAL CHEMISTRY; FLUORINE
Research-Areas	Pharmacology \& Pharmacy; Chemistry
Web-of-Science-Categories	Chemistry, Medicinal; Chemistry, Organic
Author-Email	schegolkov@ios.uran.ru
ResearcherID-Numbers	Burgart, Yanina/T-8025-2017 Shchegol'kov, Evgenii/H-6790-2015
ORCID-Numbers	Burgart, Yanina/0000-0001-6061-2410 Shchegol'kov, Evgenii/0000-0001-6611-2855
Funding-Acknowledgement	Ural Branch of the Russian Academy of Sciences {[}15-21-3-5]; Russian Foundation for Basic Research {[}14-03-31541]; Russian Science Foundation {[}16-13-10255]
Funding-Text	This work was financially supported by the Ural Branch of the Russian Academy of Sciences (Grant No. 15-21-3-5), the Russian Foundation for Basic Research {[}Grant No. 14-03-31541 for E.V. Shchegol'kov (biological and physico-chemical investigations)] and Russian Science Foundation {[}Grant No. 16-13-10255 for V.I. Saloutin (synthetic part)]. The authors are grateful for Dr. Yu.S. Kudyakova and A.N. Trefilova for assistance in manuscript preparation.
Number-of-Cited-References	29
Usage-Count-Last-180-days	2
Usage-Count-Since-2013	6
Journal-ISO	Bioorg. Med. Chem. Lett.
Doc-Delivery-Number	DJ4ZR