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Synthesis and Antimicrobial Evaluation of 2-(6-Imidazo[1,2-a]pyridin-2-yl-5-methyl-2,4-dioxo-3-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-1(2H)-yl)-N-arylacetamide Derivatives

Authors :
Sergiy V. Vlasov
Hanna I. Severina
Oleksandr V. Borysov
Konstantin Yu. Krolenko
Pavlo E. Shynkarenko
Narzullo B. Saidov
Vitaliy S. Vlasov
Victoriya A. Georgiyants
Source :
Molbank, Vol 2022, Iss 1, p M1331 (2022)
Publication Year :
2022
Publisher :
MDPI AG, 2022.

Abstract

6-Heteryl-5-methylthieno[2,3-d]pyrimidin-2,4(1H,3H)-diones are of great interest as the promising objects for the search of antibacterials. In this communication, we obtained 6-(imidazo[1,2-a]pyridin-2-yl)-5-methyl-3-phenylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione by interaction of 6-(bromoacetyl)-5-methyl-3-phenylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione with 2-aminopyridine. The obtained heterocyclic hybrid was further modified by alkylation with 2-chloroarylacetamides. Antimicrobial activity studies for the synthesized compounds using the agar well diffusion method revealed their moderate activity against S. aureus, E. coli and B. subtilis. According to the double dilution assay MIC value results for 6-(imidazo[1,2-a]pyridin-2-yl)-5-methyl-3-phenylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dioneagainst P. aeruginosa was less than the value determined for the reference drug streptomycin. The docking study of the synthesized compounds to the active site of TrmD isolated from P. aeruginosa did not show their effective inhibitory activity.

Details

Language :
English
ISSN :
14228599
Volume :
2022
Issue :
1
Database :
Directory of Open Access Journals
Journal :
Molbank
Publication Type :
Academic Journal
Accession number :
edsdoj.b2760063f9f34bc0a06ca5df2dea66f6
Document Type :
article
Full Text :
https://doi.org/10.3390/M1331