TITLE:
Synthesis and Antibacterial Activities of New 2-(Benzylthio)pyrimidines and 2-(Benzimidazolylmethylthio)pyrimidines Derivatives
AUTHORS:
Achi Patrick-Armand, Coulibali Siomenan, Zon Doumade, Timotou Adéyolé, Bolou Eric, Touré Daouda, Sissouma Drissa, Adjou Ané
KEYWORDS:
2-Thiopyrimidine, Benzylthiouracil, Benzimidazole, Antibacterial Activity
JOURNAL NAME:
Open Journal of Medicinal Chemistry,
Vol.11 No.3,
September
18,
2021
ABSTRACT: 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.