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Slavchev, Ivaylo M.; Mitrev, Yavor; Shivachev, Boris; Valcheva, Violeta; Dogonadze, Marine; Solovieva, Natalia; Vyazovaya, Anna; Mokrousov, Igor; Link, Wolfgang; Jiménez, Lucía; Cautain, Bastien; Mackenzie, Thomas A.; Portugal, Isabel; Lopes, Francisca; Capela, Rita; Perdigão, João; Dobrikov, Georgi M.

Synthesis, Characterization and Complex Evaluation of Antibacterial Activity and Cytotoxicity of New Arylmethylidene Ketones and Pyrimidines with Camphane Skeletons

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  • Media type: E-Article
  • Title: Synthesis, Characterization and Complex Evaluation of Antibacterial Activity and Cytotoxicity of New Arylmethylidene Ketones and Pyrimidines with Camphane Skeletons
  • Contributor: Slavchev, Ivaylo M.; Mitrev, Yavor; Shivachev, Boris; Valcheva, Violeta; Dogonadze, Marine; Solovieva, Natalia; Vyazovaya, Anna; Mokrousov, Igor; Link, Wolfgang; Jiménez, Lucía; Cautain, Bastien; Mackenzie, Thomas A.; Portugal, Isabel; Lopes, Francisca; Capela, Rita; Perdigão, João; Dobrikov, Georgi M.
  • imprint: Wiley, 2022
  • Published in: ChemistrySelect
  • Language: English
  • DOI: 10.1002/slct.202201339
  • ISSN: 2365-6549
  • Keywords: General Chemistry
  • Origination:
  • Footnote:
  • Description: <jats:title>Abstract</jats:title><jats:p>The synthesis of 20 arylidenecamphors and 15 pyrimidines with camphane skeleton is described in the current report. A modified method for preparation of sterically hindered 2‐aminopyrimidines in two steps was demonstrated. The evaluation of their <jats:italic>in vitro</jats:italic> activity against <jats:italic>Mycobacterium tuberculosis</jats:italic> H37Rv showed different MIC values (up to 0.91 μM for ketone <jats:bold>39</jats:bold>). Compound <jats:bold>35</jats:bold> demonstrated moderate (8.23 μM), but sustainable activity toward a collection of drug‐resistant <jats:italic>M. tuberculosis</jats:italic> strains. Many of the compounds (especially among 2‐aminopyridines <jats:bold>42</jats:bold>–<jats:bold>56</jats:bold>) exhibited good to excellent activity against different strains of pathogenic bacteria and fungi (MIC up to 0.60 μM for compound <jats:bold>50</jats:bold>), compared with reference antibiotics. Many of the newly designed compounds possess also <jats:italic>in vitro</jats:italic> cytotoxicity.</jats:p>