Author(s)

Achi Patrick-Armand¹, Coulibali Siomenan^1*, Zon Doumade², Timotou Adéyolé², Bolou Eric³, Touré Daouda⁴, Sissouma Drissa¹, Adjou Ané¹

¹Laboratoire de Constitution et Réaction de la Matière, UFR Sciences des Structures de la Matière et Technologie, Université Félix Houphouët Boigny de Cocody, Abidjan, Côte d’Ivoire.
²Département de Mathématiques-Physique-Chimie, UFR des Sciences Biologiques, Université Peleforo Gon Coulibaly, Korhogo, Côte d’Ivoire.
³Centre National de Floristique, Université Félix Houphouët-Boigny de Cocody, Abidjan, Côte d’Ivoire.
⁴Département de Biochimie-Génétique, UFR des Sciences Biologiques, Université Peleforo Gon Coulibaly, Korhogo, Côte d’Ivoire.

A series of 2-(benzylthio)pyrimidines (6a-l) and 2-(benzimidazolylmethylthio)-pyrimidines derivatives (6m and 6n) analogues of ethyl 2-(benzylthio)-6-methyl-4-phenyl-1,4-dihydropyrimidine-5-carboxylates and ethyl 2-(((1H-benzimidazol-2-yl)methyl)thio)-6-methyl-4-phenyl-1,4-dihydropyri-midine-5-carboxylates were prepared and evaluated for antibacterial activity. These compounds were obtained by condensation of 2-thiopyrimidines (4) with benzyl halides or 2-(chloromethyl)-1H-benzimidazole (5) in the presence of a base. All compounds were characterized by ¹H, ¹³C and HRMS spectra. Out of fourteen, only eight compounds were screened against multi-resistant strains of Escherichia coli and Staphylococcus aureus. The results revealed that all of them were found to possess significant antibacterial activity against the germs tested. Compounds 6c, 6d, 6h and 6m were more active on S. aureus and compounds 6h and 6m more active on E. coli.

2-Thiopyrimidine, Benzylthiouracil, Benzimidazole, Antibacterial Activity

Patrick-Armand, A. , Siomenan, C. , Doumade, Z. , Adéyolé, T. , Eric, B. , Daouda, T. , Drissa, S. and Ané, A. (2021) Synthesis and Antibacterial Activities of New 2-(Benzylthio)pyrimidines and 2-(Benzimidazolylmethylthio)pyrimidines Derivatives. Open Journal of Medicinal Chemistry, 11, 27-39. doi: 10.4236/ojmc.2021.113003.