- Synthesis, molecular docking and antimicrobial activity of new fused pyrimidine and pyridine derivatives
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Synthesis of some new heterocyclic ring systems incorporated pyrimidine and pyridine moieties starting from 1-(furan-2-yl)-3-(thiophen-2-yl) chalcone was achieved. The structure of the new compounds was interpreted by spectral studies and ESI-MS analysis.
- Radwan, Mohamed A.A.,Alshubramy, Maha A.,Abdel-Motaal, Marwa,Hemdan, Bahaa A.,El-Kady, Dina S.
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- Triethylamin-mediated addition of 2-aminoethanethiol hydrochloride to chalcones: Synthesis of 3-(2-aminoethylthio)-1-(aryl)-3-(thiophen-2-yl) propan-1-ones and 5,7-diaryl-2,3,6, 7-tetrahydro-1,4-thiazepines
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The triethylamin-mediated addition of 2-aminoethanethiol hydrochloride to chalcone analogs was investigated. This addition, bearing a 2-thienyl group at the 3-position, gave the only addition adduct at room temperature in 3 h, whereas the chalcones bearing the 2-furyl group at the 1-position gave an addition-cyclization product (1, 4-thiazepine) in the same conditions. The effect of the groups to the reaction was investigated by changing the 1- and 3-position groups. The chalcones bearing the 2-thienyl group at the 1-position and the others afforded the mixture of products in different ratio at rt for 0.5-24 h. Moreover, the addition-cyclization products (1,4-thiazepine) were obtained under reflux conditions in 36 h. The structures of the synthesized compounds were elucidated by 1H NMR, 13C NMR, infrared, and elemental analysis.
- Gürdere, Meliha Burcu,Eme?, Ali Cemal,Aslan, Osman Nuri,Budak, Yakup,Ceylan, Mustafa
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p. 536 - 545
(2016/05/02)
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- Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation, and ulcerogenic liability of new 1,3,5-triarylpyrazoline derivatives possessing a methanesulfonyl pharmacophore
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A new series of 1,3,5-triarylpyrazolines 13a–l was synthesized and all prepared compounds were evaluated for their in vitro COX-1/COX-2 inhibitory activity and in vivo anti-inflammatory activity. All test compounds were more selective for the COX-2 isozyme and showed good in vivo anti-inflammatory activity. Compound 13h was the most COX-2 selective compound (COX-2 selectivity index (SI)=10.23) and the most potent anti-inflammatory derivative (ED50-60.1μmol/kg) in comparison with celecoxib (COX-2 SI=9.29 and ED50=81.4μmol/kg). All screened compounds were less ulcerogenic (ulcer indexes (UI)=0.33–1.33) than aspirin (UI=2.33) and comparable to celecoxib (UI=0.33).
- Abdellatif, Khaled R. A.,Fadaly, Wael A. A.,Azouz, Amany A.
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- Synthesis, characterization, and antibacterial activity of novel pyridones
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Novel ethyl 2-oxo-4,6-diaryl-1,2,3,4-tetrahydropyridine-3-carboxylate and 4,6-diaryl-3,4-dihydropyridine-2(1H)-one derivatives have been synthesized from the cyclization of adducts of diethylmalonate to chalcones with ammonium acetate. The structures were established on the basis of extensive spectroscopic methods and further confirmed by X-ray crystallographic analysis. Antibacterial activity of obtained pyridones was investigated against four human pathogen microorganisms and the compounds showed poor activity.
- Gezegen, Hayreddin,Ceylan, Mustafa,Karaman, Isa,?ahin, Ertan
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p. 1084 - 1093
(2014/04/03)
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- Atom-efficient, solvent-free, green synthesis of chalcones by grinding
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An improved Claisen-Schmidt condensation reaction of methyl ketones and aromatic aldehydes can be achieved by grinding at room temperature in the absence of solvents. This process is simple, efficient, economical, and environmentally benign compared to classical reactions.
- Rateb, Nora M.,Zohdi, Hussein F.
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experimental part
p. 2789 - 2794
(2009/12/06)
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- Synthesis of 3-Cyano-2-methylpyridines Substituted with Heteroaromatics
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A series of title compounds were easily prepared by the sonication of α,β-unsaturated carbonyl compound in acetonitril in the presence of potassium t-butoxide.
- Shibata, Katsuyoshi,Katsuyama, Isamu,Matsui, Masaki,Muramatsu, Hiroshiga
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p. 161 - 165
(2007/10/02)
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- Heterocycles. 3. Synthesis and Spectral Data of Some 2-Pyrazolines
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The reaction of 1,3-diaryl-2-propen-1-ones (Ia-o) with hydrazine and methyl- and phenylhydrazine produced different substituted 2-pyrazolines (III).The structures of these products were evident from their chemical and spectroscopic analysis.
- El-Rayyes, Nizar R.,Hovakeemian, George H.,Hmoud, Hayat S.
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p. 225 - 229
(2007/10/02)
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