Ozer, Erdem KamilGunduz, Miyase GozdeEl-Khouly, AhmedSara, Mehmet YildirimSimsek, RahimeIskit, Alper BektasSafak, Osman Cihat2020-03-262020-03-2620151300-0527https://dx.doi.org/10.3906/kim-1412-72https://hdl.handle.net/20.500.12395/32324This 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.en10.3906/kim-1412-72info:eu-repo/semantics/openAccess1,4-Dihydropyridinehexahydroquinolinesynthesiscalcium channelArticle394886896Q3WOS:000359063900017Q3