Synthesis and antimicrobial activity of some new pyrrole derivatives

New pyrrole derivatives were synthesized and structures were confirmed by IR, 1H NMR, 13C NMR, mass spectra, and elemental analyses data. The reaction was performed by using ordinary condensation type, which enabled to easy work-up and good yield. Synthesized compounds were screened for antimicrobial activity.DOI: http://dx.doi.org/10.4314/bcse.v26i3.1

Ethyl 3,5-Dimethyl-4-[(4-phenyl-1,3-thiazol-2-yl)carbamoyl]-1H-pyrrole-2-carboxylate

A new compound, ethyl 3,5-dimethyl-4-[(4-phenyl-1,3-thiazol-2-yl)carbamoyl]-1H-pyrrole-2-carboxylate (3) was synthesized by the amination method. The synthesized compound (3) was characterized by IR, 1H-NMR, 13C-NMR, mass spectral data and elemental analysis

Tyrosinase enzyme mediated: Synthesis and larvicidal activity of 1,5-diphenyl pent-4-en-1-one derivatives against Culex quinquefasciatus and investigation of Ichthyotoxicity against O. mossambicus

Abstract Larvicidal activity of 1,5-diphenylpent-4-en-1-one derivatives were synthesized via grindstone method, tyrosinase enzyme used as a catalyst of this process. This method offers high yields with mild reaction conditions. Synthesized compounds were conformed from FTIR, 1H NMR, 13C NMR, mass spectral and elemental analysis. In this study, a total of 17 compounds (1a–1q) were synthesized, and their larvicidal and antifeedant activities were evaluated. Compound 1i (1-(5-oxo-1,5-diphenylpent-1-en-3-yl)-3-(3-phenylallylidene)thiourea) was extremely active (LD50: 12.09 µg/mL) against Culex quinquefasciatus compared with temephos and permethrin, whereas compounds 1i at 100 µg/mL generated 0% mortality within 24h against Oreochromis mossambicus in an antifeedant screening, and Ichthyotoxicity was determined as the death ratio (%) at 24 h. The compounds 1a, 1e, 1f, 1j, and 1k were found to be highly toxic whereas the 1i was not toxic in antifeedant screening. Therefore, 1i was found to have a high larvicidal activity against C. quinquefasciatus, and was non-toxic to non-target aquatic species. Molecular docking studies also supported the finding that 1i is a potent larvicide with more binding energy than the control (-10.0 vs. -7.6 Kcal/mol) in the 3OGN protein. The lead molecule is very important to larvicidal properties and insecticides.</jats:p