الفهرس | Only 14 pages are availabe for public view |
Abstract Part 1: A new series of bis(4H-chromene), bis(pyrano[3,2-c]chromene), and bis(pyrano[2,3-c]pyrazole) each linked to the piperazine core via ether linkages was synthesized. The target compounds are probably formed through a three-component reaction involving two equivalents of each malononitrile and the corresponding active methylene compounds, such as dimedone, 4-hydroxycoumarine, or 5-methyl- 2,4-dihydro-3H-pyrazol-3-one. Several spectral methods and elemental analyses were used to deduce the chemical structures of the novel compounds. Furthermore, all synthesized compounds were tested for antimicrobial activity, which revealed promising inhibitory results against a variety of multidrugresistant microbial strains. These findings were compared to those obtained in the in silico molecular docking study. Part 2: The molecular hybridization of various compounds with known pharmacological activity is a particularly popular approach for the development of potential drugs with improved pharmacokinetic profiles. In this respect, a novel series of bis(1,4-dihydropyridine-3,5-dicarbonitrile), bis(decahydroacridine), bis(tetrahydrodipyrazolo[3,4-b:4’,3’-e]pyridin), tetrahydropyrimido[4,5- b]quinoline, and bis(tetrahydropyrimido[4,5-b]quinoline-2,4,6-trione) derivatives linked to piperazine core via phenoxyethanone linkages were prepared via Hantzsch like reaction of the ((piperazine-1,4- diylbis(2-oxoethane-2,1-diyl))bis(oxy))dibenzaldehydes, with the appropriate active methylene containing reagents. Attempted synthesis of the target products via bis-alkylation of the appropriate phenol with 1,1’-(piperazine-1,4-diyl)bis(2-chloroethan-1-one) in different basic conditions were unsuccessful. |