Foroumadi A, Analuie N, Rezvanipour M, Sepehri G, Najafipour H, Sepehri H, Javanmardi K, Esmaeeli F
Kerman University of Medical Sciences, Research Center, Iran.
Farmaco. 2002 Mar;57(3):195-9. doi: 10.1016/s0014-827x(01)01191-0.
Various diester analogues of nifedipine, in which the orthonitrophenyl group at position 4 is replaced by 1-methyl-2-methylthio-5-imidazolyl substituent, were synthesized and evaluated as calcium channel antagonists on guinea-pig ileal smooth muscle. Nifedipine was used as standard. Comparison of the activities of symmetrical esters (3a-e) indicate that increasing the length of alkyl chain in C3 and C5 ester substituents increases the antagonist activity and the n-propyl ester being preferred (IC50= 2.66 x 10(-9) M). In asymmetrical series (6a-g), compound 6g having ethyl and n-butyl ester at C3 and C5 positions of basic dihydropyridine structure was found to be the most active (IC50= 1.32 x 10(-9) M).
合成了硝苯地平的各种二酯类似物，其中4位的邻硝基苯基被1-甲基-2-甲硫基-5-咪唑基取代基取代，并在豚鼠回肠平滑肌上作为钙通道拮抗剂进行了评估。硝苯地平用作标准品。对称酯（3a-e）活性的比较表明，增加C3和C5酯取代基中烷基链的长度会增加拮抗剂活性，正丙酯为首选（IC50 = 2.66×10（-9）M）。在不对称系列（6a-g）中，发现在碱性二氢吡啶结构的C3和C5位置具有乙酯和正丁酯的化合物6g活性最高（IC50 = 1.32×10（-9）M）。
