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

6-Heteryl-5-methylthieno[2,3-<i>d</i>]pyrimidin-2,4(1<i>H</i>,3<i>H</i>)-diones are of great interest as the promising objects for the search of antibacterials. In this communication, we obtained 6-(imidazo[1,2-<i>a</i>]pyridin-2-yl)-5-methyl-3-phenylt...

Deskribapen osoa

Xehetasun bibliografikoak
Egile Nagusiak: Sergiy V. Vlasov, Hanna I. Severina, Oleksandr V. Borysov, Konstantin Yu. Krolenko, Pavlo E. Shynkarenko, Narzullo B. Saidov, Vitaliy S. Vlasov, Victoriya A. Georgiyants
Formatua: Artikulua
Hizkuntza:English
Argitaratua: MDPI AG 2022-02-01
Saila:Molbank
Gaiak:
Sarrera elektronikoa:https://www.mdpi.com/1422-8599/2022/1/M1331
Deskribapena
Gaia:6-Heteryl-5-methylthieno[2,3-<i>d</i>]pyrimidin-2,4(1<i>H</i>,3<i>H</i>)-diones are of great interest as the promising objects for the search of antibacterials. In this communication, we obtained 6-(imidazo[1,2-<i>a</i>]pyridin-2-yl)-5-methyl-3-phenylthieno[2,3-<i>d</i>]pyrimidine-2,4(1<i>H</i>,3<i>H</i>)-dione by interaction of 6-(bromoacetyl)-5-methyl-3-phenylthieno[2,3-<i>d</i>]pyrimidine-2,4(1<i>H</i>,3<i>H</i>)-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 <i>S. aureus</i>, <i>E. coli</i> and <i>B. subtilis</i>. According to the double dilution assay MIC value results for 6-(imidazo[1,2-<i>a</i>]pyridin-2-yl)-5-methyl-3-phenylthieno[2,3-<i>d</i>]pyrimidine-2,4(1<i>H</i>,3<i>H</i>)-dioneagainst <i>P. aeruginosa</i> 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 <i>P. aeruginosa</i> did not show their effective inhibitory activity.
ISSN:1422-8599