Luo Y L, Yang Z X, Peng S X
Division of Medicinal Chemistry, China Pharmaceutical University, Nanjing.
Yao Xue Xue Bao. 1990;25(5):374-8.
N-(2-mercaptopyridyl-3-formyl)-N-alkyl glycine I1-8) were synthesized by the condensation of 2-mercaptopyridyl-3-formyl chloride with ethyl N-alkyl glycinate followed by hydrolysis. The corresponding disulfides (II1-7) were obtained by the oxidation of compounds I1-7 with hydrogen peroxide (1%) in weak alkali medium below 10 degrees C. In preliminary tests, some compounds showed inhibitory activity of ACE in vitro.
通过2-巯基吡啶-3-甲酰氯与N-烷基甘氨酸乙酯缩合然后水解合成了N-(2-巯基吡啶基-3-甲酰基)-N-烷基甘氨酸(I1-8)。相应的二硫化物(II1-7)是通过在10℃以下的弱碱性介质中用过氧化氢(1%)氧化化合物I1-7得到的。在初步试验中,一些化合物在体外显示出对ACE的抑制活性。