Synthesis of fused 1,4-dihydropyridines as potential calcium channel blockers

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dc.contributor.authorOzer, Erdem Kamil
dc.contributor.authorGunduz, Miyase Gozde
dc.contributor.authorEl-Khouly, Ahmed
dc.contributor.authorSara, Yildirim
dc.contributor.authorSimsek, Rahime
dc.contributor.authorIskit, Alper Bektas
dc.contributor.authorSafak, Cihat
dc.date.accessioned2020-03-26T19:55:51Z
dc.date.available2020-03-26T19:55:51Z
dc.date.issued2018
dc.departmentSelçuk Üniversitesien_US
dc.description.abstractObjective: 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.en_US
dc.description.sponsorshipTurkish Academy of SciencesTurkish Academy of Sciences [EA-TUBA-GEBIP/2001-2-11]en_US
dc.description.sponsorshipAlper B. Iskit has been supported by the Turkish Academy of Sciences, in the framework of the Young Scientist Award Program (EA-TUBA-GEBIP/2001-2-11).en_US
dc.identifier.doi10.1515/tjb-2016-0247en_US
dc.identifier.endpage586en_US
dc.identifier.issn0250-4685en_US
dc.identifier.issn1303-829Xen_US
dc.identifier.issue6en_US
dc.identifier.scopusqualityQ4en_US
dc.identifier.startpage578en_US
dc.identifier.urihttps://dx.doi.org/10.1515/tjb-2016-0247
dc.identifier.urihttps://hdl.handle.net/20.500.12395/36973
dc.identifier.volume43en_US
dc.identifier.wosWOS:000450015000002en_US
dc.identifier.wosqualityQ4en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakTR-Dizinen_US
dc.language.isoenen_US
dc.publisherWALTER DE GRUYTER GMBHen_US
dc.relation.ispartofTURKISH JOURNAL OF BIOCHEMISTRY-TURK BIYOKIMYA DERGISIen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.selcuk20240510_oaigen_US
dc.subject1,4-Dihydropyridineen_US
dc.subjectCalcium channelen_US
dc.subjectHexahydroquinolineen_US
dc.subjectIsolated aortic ringsen_US
dc.subjectRelaxant effectsen_US
dc.titleSynthesis of fused 1,4-dihydropyridines as potential calcium channel blockersen_US
dc.typeArticleen_US

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