1448439-61-9Relevant academic research and scientific papers
Synthesis and antimicrobial evaluation of new 2-pyridinone and 2-iminochromene derivatives containing morpholine moiety
Salem, Mohamed A.,Abbas, Samir Y.,Helal, Mohamed H.,Alzahrani, Abdullah Y.
, p. 2117 - 2123 (2021)
As trail to overcome on the antimicrobial drug-resistance problems, new functionalized 2-pyridinone and 2-iminochromene derivatives bearing morpholine moiety were designed and synthesized. The 2-pyridinone derivatives were obtained through the cyclization of cyanoacetohydrazone of 4-morpholinylacetophenone with 1,3-dicarbonyl compounds, α,β-unsaturated nitriles or 2-(arylidene)malononitriles. The 2-iminochromene derivatives were synthesized through the ring closure of cyanoacetohydrazonewith salicylaldehyde derivatives. The antibacterial and antifungal activities for the synthesized 2-pyridinone and 2-iminochromene derivatives were investigated. Most of the tested compounds showed moderate activity against P. vulgaris. Compounds 4a,b and 5a,b showed moderate activity against G ?ve bacteria. All iminochromene derivatives showed moderate activity against C. albicans. Compound 8c was the most active compound.
Design, synthesis and anticancer activity of new 3-cyano-2 (1H)-pyridone and 3-cyanopyridine-2-(1H)-thione derivatives
Motaal, E. A. Abdel,El-Gaby,Salem
, p. 875 - 884 (2015/10/28)
The main objective of the present research study is to synthesize some novel chalcone, cyanoacetohydrazone, enaminone, 3-cyano-2(1H)-pyridone and 3-cyanopyridine-2-(1H)-thione derivatives and evaluate them for their anticancer effect. The novel chalcones 2a-c were achieved by Claisen-Schmidt condensation of appropriate benzaldehydes with ethanone derivative 1. Treatment of cyanoacetic acid hydrazide with ethanone derivative 1 yielded the correspondinghydrazone derivative 3. Condensation of ethanone derivative 1 with DMF-DMA afforded (E)-3-(dimethylamino)-1-(4-morpholinophenyl)prop-2-en-1-one 4. Heterocyclization of chalcones 2a-c with cyanothioacetamide yielded 2-thioxo-1,2-dihydropyridine-3-carbonitriles 7ac. In a similar manner, cyclocondensation of chalcones 2a, b with cyanoacetamide afforded the corresponding 2-oxo-1,2-dihydropyridine-3-carbonitriles 8a, b. The Reaction of compound 2a with ethyl cyanoacetate furnished 2-oxo-1,2-dihydropyridine-3-carboxylate 12. The 2-oxo-4-phenyl-1,2-dihydro-pyridine-3,5-dicarbonitriles 14a, b were obtained by cyclization of cyanoacetohydrazone 3 with cinnamonitriles. The structures of the synthesized compounds were confirmed by elemental analysis, mass spectrometry, IR and 1H-NMR spectroscopy. The anticancer activity of the newly synthesized compounds was screened in vitro against Human lung carcinoma (A 549) cell line indicating that compounds 7b and 8a possess the most potent inhibitory effect against the human lung carcinoma cell line (A549).
Synthesis and biological evaluation of some novel thiazole compounds as potential anti-inflammatory agents
Helal,Salem,El-Gaby,Aljahdali
, p. 517 - 526 (2013/10/01)
In the present investigation, furo[2,3-d]thiazol-5(2H)-one 5 was obtained from reaction of thiosemicarbazone derivative 2 with diethyl acetylene dicarboxylate. A series of newly synthesized 2-(hydrazinyl)thiazol-4(5H)-one 6, 7 & 8 and 2-(4-(substituted)-thiazol-2-yl)hydrazono derivatives 9a, b & 10 were synthesized from treatment of thiosemicarbazone derivative 2 with appropriate α-halogenated compounds. Also, a one pot synthesis of thiazole derivatives 13 & 15 was achieved from three components reaction of hydrazone derivative 11 with phenyl isothiocyanate and α-halogenated compounds catalyzed by DMF/KOH. 4-(4-Morpholino phenyl) thiazol-2-amino 17 was obtained via the reaction of acetophenone derivative 1 with thiourea in presence of iodine. The reactivity of 2-aminothiazole 17 toward some electrophilic reagents was investigated. The structure of the newly compounds was confirmed on the basis of elemental analysis and spectral data. The antibacterial activity towards two Gram negative (Proteus mirabilis & Serratia marcesens) and two Gram positive (Staphylococcus aureus & Bacillus cereus) bacteria was investigated. The anti-inflammatory activity was also investigated and the inhibition of the carrageenin-induced oedema by these compounds was established.
