Zarghi A, Derakhshandeh K, Roshanzamir F, Jorjani M, Rastegar H, Varmazyari M, Shafiee A
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Shaheed Beheshti University of Medical Sciences, Tehran, Iran.
Boll Chim Farm. 2002 Jan-Feb;141(1):15-20.
New alkyl ester analogues of nifedipine, in which the ortho-nitrophenyl group of position 4 is replaced by 1-(4-nitrobenzyl)-5-imidazolyl or 2-methylthio-1-(4-nitrobenzyl)-5-imidazolyl substituent, were synthesized and evaluated as calcium-channel antagonists using the electrically induced contraction of guinea-pig ileal longitudinal smooth muscle. Our results demonstrate that all compounds inhibited the contractile response of guinea-pig ileum to electrical stimulation and the IC50 value of the most potent compounds 6a and 6f were significantly lower than that of nifedipine. Therefore, they are more potent than nifedipine.
合成了硝苯地平的新型烷基酯类似物，其中4位的邻硝基苯基被1-(4-硝基苄基)-5-咪唑基或2-甲硫基-1-(4-硝基苄基)-5-咪唑基取代基所取代，并利用豚鼠回肠纵行平滑肌的电诱导收缩来评估其作为钙通道拮抗剂的活性。我们的结果表明，所有化合物均抑制豚鼠回肠对电刺激的收缩反应，且最有效的化合物6a和6f的IC50值显著低于硝苯地平。因此，它们比硝苯地平更有效。
