Kondanse 1,4-Dihidropiridin-3-Karboksilat Türevleri ve Kalsiyum Modülatör Etkileri

Abstract

In this study sixteen 2,6,6-trimethyl-4-aryl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate (compound 1-16) have been synthesized. The synthesis of the compounds was realised by the reaction of the 4,4-dimethyl-1,3-cyclohexanedione, appropriate acetoacetate derivates and naphthalene carbaldehyde in the presence of ammonium acetate in methanol. The structure of the compounds were confirmed by IR, 1H-NMR, 13C-NMR, mass spectroscopy and elemental analyses. The structure of the compound 10 was also elucidated by COSY and X-Ray analyses. Calcium modulatory activity of the compounds were determined by the tests performed on the isolated rabbit gastric fundus strips of smooth muscle by using nifedipine as standart. When results were investigated; while ECmax values of compounds 2, 6 and 14 are close to that of nifedipine, pD2 values of them have been found lower than that of nifedipine. It is thought that the relaxant activity of synthesised compound have shown calcium channel blockage effect as nifedipine. The activity results have been found statistically significant.