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

• Autor(a) principal: Slavchev, Ivaylo M.
• Data de Publicação: 2022
• Outros Autores: 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.
• Tipo de documento: Artigo
• Idioma: eng
• Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
• Texto Completo: http://hdl.handle.net/10451/58922
• topic: antibiotics; camphor; cytotoxicity; drug-discovery; heterocycles; tuberculosi

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 in vitro activity against Mycobacterium tuberculosis H37Rv showed different MIC values (up to 0.91 μM for ketone 39). Compound 35 demonstrated moderate (8.23 μM), but sustainable activity toward a collection of drug-resistant M. tuberculosis strains. Many of the compounds (especially among 2-aminopyridines 42–56) exhibited good to excellent activity against different strains of pathogenic bacteria and fungi (MIC up to 0.60 μM for compound 50), compared with reference antibiotics. Many of the newly designed compounds possess also in vitro cytotoxicity.