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    Microwave-assisted synthesis of condensed 1,4-dihydropyridines as potential calcium channel modulators
    (SCIENTIFIC TECHNICAL RESEARCH COUNCIL TURKEY-TUBITAK, 2015) Ozer, Erdem Kamil; Gunduz, Miyase Gozde; El-Khouly, Ahmed; Sara, Mehmet Yildirim; Simsek, Rahime; Iskit, Alper Bektas; Safak, Osman Cihat
    This study reports the design, synthesis, and calcium channel modulatory activity evaluation of a series of 14 novel fused 1,4-dihydropyridine derivatives. The molecular design of the compounds was based on modifications of nifedipine, which is a calcium channel blocker. The compounds were achieved by one-pot microwave-assisted reaction of 4,4-dimethyl-1,3-cyclohexanedione, 5-chlorosalicylaldehyde/3,5-dichlorosalicylaldehyde, an appropriate alkyl acetoacetate, and ammonium acetate in ethanol according to a modified Hantzsch reaction. The structures of the compounds were confirmed by spectral methods and elemental analysis. To evaluate their relaxant activities, the maximum relaxant response (E-max) and pD(2) values of the compounds and nifedipine were determined on isolated rat aorta rings. The obtained results indicated that all compounds produced concentration-dependent relaxation on the rings possibly due to the blockade of calcium channels. The E-max values (a measure of efficacy) of five compounds were higher than those of nifedipine.
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    Synthesis of fused 1,4-dihydropyridines as potential calcium channel blockers
    (WALTER DE GRUYTER GMBH, 2018) Ozer, Erdem Kamil; Gunduz, Miyase Gozde; El-Khouly, Ahmed; Sara, Yildirim; Simsek, Rahime; Iskit, Alper Bektas; Safak, Cihat
    Objective: The aim of this study was to synthesize ten 1,4-dihydropyridine (DHP) derivatives in which substituted cyclohexane rings were fused to the DHP ring and to determine how different ester groups and the benzoyl substituent introduced in 4-phenyl ring affected their calcium channel blocking activity. Methods: A microwave-assisted one-pot method was applied for the synthesis of compound 1-5 according to a modified Hantzsch reaction. The benzoyl moiety was introduced in the 4-phenyl ring of these dihydropyridines by refluxing with benzoyl chloride in acetone in the presence of anhydrous potassium carbonate. Synthesized products were characterized by elemental analysis, IR, H-1-NMR and C-13-NMR spectroscopy. The inhibitory actions of compounds 1-10 on calcium channel blocking activity were tested on isolated rat aorta preparations. Results: The obtained pharmacological results showed that although all compounds are potent relaxing agents on isolated rat aorta smooth muscle, introduction of a benzoyloxy substitiuent on the phenyl ring (compound 6-10) decreased the relaxant effect of these compunds. Conclusion: The reported 1,4-DHP derivatives have calcium channel blocking activity on rat aorta smooth muscle.