4-tetrahydronaphthyl)acetyl]-L- thioprolyl]thiazolidine (13) exhibited an approximately 20-fold (IC50 = 2.3 nm) increase in potency compared with 1. Compounds having a formyl or a cyano group showed much more potent inhibitory activities than those which lack such a functional group. Among all compounds tested in vitro, 1-[1-(2-indanylacetyl)-L-prolyl]prolinal (27), 1-[1-[(S)-2-(1,2,3,4-tetrahydronaphthyl)acetyl]-L-
通过对1- [1-(4-苯基丁酰基)-L-脯
氨酰基]-
吡咯烷(SU
AM-1221,1)或1- [1-(苄氧羰基)-
L-脯氨酸]脯
氨酸(Z- Pro-proalal,2)和被测试对犬脑中纯化的脯
氨酰内肽酶(PEP)的体外抑制活性。在一系列缺少甲酰基或
氰基的化合物中,3- [3-[(S)-2-(
1,2,3,4-四氢萘基)乙酰基] -L-
硫代脯
氨酰基]
噻唑烷(13)与1相比,效价提高了约20倍(IC50 = 2.3 nm)。具有甲酰基或
氰基的化合物显示出比没有这种官能团的化合物更有效的抑制活性。在体外测试的所有化合物中,1- [1-(2-
茚满基乙酰基)-L-脯
氨酰基]脯
氨酸(27),1- [1-[(S)-2-(
1,2,3,4-四氢萘基)乙酰基] -L-脯
氨酰]脯
氨酸(29),1- [3-[(S)-2-(1,2,3,