Synthesis and antibacterial evaluation of novel 1-(2,6-diethylphenyl)-5-oxopyrrolidine derivatives

Mindaugas Žukauskas; Birutė Grybaitė; Rita Vaickelionienė; Giedrius Vaickelionis; Jūratė Šiugždaitė; Vytautas Mickevičius

doi:10.6001/chemija.v31i4.4327

Mindaugas Žukauskas
Birutė Grybaitė
Rita Vaickelionienė
Giedrius Vaickelionis
Jūratė Šiugždaitė
Vytautas Mickevičius

DOI: https://doi.org/10.6001/chemija.v31i4.4327

Keywords: 5-oxopyrrolidines, hydrazones, azoles, antibacterial activity

Abstract

Synthesis of 1-(2,6-diethylphenyl)-5-oxopyrrolidine derivatives containing hydrazone, semi/thiosemicarbazide and azole moieties is described. For this purpose, the appropriate hydrazide was treated with aromatic aldehydes, ketones and phenyl iso(thio)cyanates to obtain the desired outcome. The synthesized target compounds were evaluated for their antibacterial properties. The antibacterial screening revealed promising compounds with a pyrazole and thiosemicarbazide moieties in the molecule, which in some cases appeared to be 4 times more effective than Ampicillin.