Microwave-assisted synthesis of condensed 1,4-dihydropyridines as potential calcium channel modulators

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dc.contributor.authorOzer, Erdem Kamil
dc.contributor.authorGunduz, Miyase Gozde
dc.contributor.authorEl-Khouly, Ahmed
dc.contributor.authorSara, Mehmet Yildirim
dc.contributor.authorSimsek, Rahime
dc.contributor.authorIskit, Alper Bektas
dc.contributor.authorSafak, Osman Cihat
dc.date.accessioned2020-03-26T19:06:20Z
dc.date.available2020-03-26T19:06:20Z
dc.date.issued2015
dc.departmentSelçuk Üniversitesien_US
dc.description.abstractThis 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.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.doi10.3906/kim-1412-72en_US
dc.identifier.endpage896en_US
dc.identifier.issn1300-0527en_US
dc.identifier.issue4en_US
dc.identifier.scopusqualityQ3en_US
dc.identifier.startpage886en_US
dc.identifier.urihttps://dx.doi.org/10.3906/kim-1412-72
dc.identifier.urihttps://hdl.handle.net/20.500.12395/32324
dc.identifier.volume39en_US
dc.identifier.wosWOS:000359063900017en_US
dc.identifier.wosqualityQ3en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakTR-Dizinen_US
dc.language.isoenen_US
dc.publisherSCIENTIFIC TECHNICAL RESEARCH COUNCIL TURKEY-TUBITAKen_US
dc.relation.ispartofTURKISH JOURNAL OF CHEMISTRYen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.selcuk20240510_oaigen_US
dc.subject1,4-Dihydropyridineen_US
dc.subjecthexahydroquinolineen_US
dc.subjectsynthesisen_US
dc.subjectcalcium channelen_US
dc.titleMicrowave-assisted synthesis of condensed 1,4-dihydropyridines as potential calcium channel modulatorsen_US
dc.typeArticleen_US

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