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 |
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| container_issue | 10 |
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| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 26 |
| creator | Shchegol’kov, Evgeny V. Shchur, Irina V. Burgart, Yanina V. Saloutin, Victor I. Solodnikov, Sergey Yu Krasnykh, Olga P. Kravchenko, Marionella A. |
| description | [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. |
| doi_str_mv | 10.1016/j.bmcl.2016.03.107 |
| format | Article |
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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.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2016.03.107</identifier><identifier>PMID: 27072906</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>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</subject><ispartof>Bioorganic & medicinal chemistry letters, 2016-05, Vol.26 (10), p.2455-2458</ispartof><rights>2016 Elsevier Ltd</rights><rights>Copyright © 2016 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c389t-2e62c834f8ca54cfff61d6bc40906f7540f868beee3c64c49ff2006f0dd6c6823</citedby><cites>FETCH-LOGICAL-c389t-2e62c834f8ca54cfff61d6bc40906f7540f868beee3c64c49ff2006f0dd6c6823</cites><orcidid>0000-0001-6611-2855</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.bmcl.2016.03.107$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>315,781,785,3551,27928,27929,45999</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/27072906$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Shchegol’kov, Evgeny V.</creatorcontrib><creatorcontrib>Shchur, Irina V.</creatorcontrib><creatorcontrib>Burgart, Yanina V.</creatorcontrib><creatorcontrib>Saloutin, Victor I.</creatorcontrib><creatorcontrib>Solodnikov, Sergey Yu</creatorcontrib><creatorcontrib>Krasnykh, Olga P.</creatorcontrib><creatorcontrib>Kravchenko, Marionella A.</creatorcontrib><title>A convenient and efficient approach to polyfluorosalicylic acids and their tuberculostatic activity</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>[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. 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Shchur, Irina V. ; Burgart, Yanina V. ; Saloutin, Victor I. ; Solodnikov, Sergey Yu ; Krasnykh, Olga P. ; Kravchenko, Marionella A.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c389t-2e62c834f8ca54cfff61d6bc40906f7540f868beee3c64c49ff2006f0dd6c6823</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2016</creationdate><topic>Anti-mycobacterial activity</topic><topic>Antitubercular Agents - chemical synthesis</topic><topic>Antitubercular Agents - chemistry</topic><topic>Antitubercular Agents - pharmacology</topic><topic>Chemistry Techniques, Synthetic</topic><topic>Drug Evaluation, Preclinical - methods</topic><topic>Fluorine - chemistry</topic><topic>Magnesium Compounds - chemistry</topic><topic>Microbial Sensitivity Tests</topic><topic>Molecular Structure</topic><topic>Mycobacterium tuberculosis - drug effects</topic><topic>Nucleophilic substitution</topic><topic>Polyfluorosalicylic acid</topic><topic>Salicylic Acid - chemistry</topic><topic>Toxicity</topic><topic>Tuberculosis</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Shchegol’kov, Evgeny V.</creatorcontrib><creatorcontrib>Shchur, Irina V.</creatorcontrib><creatorcontrib>Burgart, Yanina V.</creatorcontrib><creatorcontrib>Saloutin, Victor I.</creatorcontrib><creatorcontrib>Solodnikov, Sergey Yu</creatorcontrib><creatorcontrib>Krasnykh, Olga P.</creatorcontrib><creatorcontrib>Kravchenko, Marionella A.</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><collection>Bacteriology Abstracts (Microbiology B)</collection><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Environmental Sciences and Pollution Management</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Shchegol’kov, Evgeny V.</au><au>Shchur, Irina V.</au><au>Burgart, Yanina V.</au><au>Saloutin, Victor I.</au><au>Solodnikov, Sergey Yu</au><au>Krasnykh, Olga P.</au><au>Kravchenko, Marionella A.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>A convenient and efficient approach to polyfluorosalicylic acids and their tuberculostatic activity</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2016-05-15</date><risdate>2016</risdate><volume>26</volume><issue>10</issue><spage>2455</spage><epage>2458</epage><pages>2455-2458</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>[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.</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>27072906</pmid><doi>10.1016/j.bmcl.2016.03.107</doi><tpages>4</tpages><orcidid>https://orcid.org/0000-0001-6611-2855</orcidid></addata></record> |
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| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2016-05, Vol.26 (10), p.2455-2458 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | MEDLINE; Access via ScienceDirect (Elsevier) |
| subjects | 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 |
| title | A convenient and efficient approach to polyfluorosalicylic acids and their tuberculostatic activity |
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