New prolyl oligopeptidase inhibitors developed from dicarboxylic acid bis (l-prolyl-pyrrolidine) amides

…, JAM Christiaans, EM Jarho, MM Forsberg…

Index: Wallen, Erik A.A.; Christiaans, Johannes A.M.; Saario, Susanna M.; Forsberg, Markus M.; Venaelaeinen, Jarkko I.; Paso, Hanna M.; Maennistoe, Pekka T.; Gynther, Jukka Bioorganic and Medicinal Chemistry, 2002 , vol. 10, # 7 p. 2199 - 2206

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Citation Number: 25

Abstract

Isophthalic acid bis (l-prolyl-pyrrolidine) amide is a very potent prolyl oligopeptidase inhibitor, but it has a log P value of-0.2, which is very low for a compound targeted to the brain. Therefore, these types of compounds were further modified to improve the structure- activity relationships, with the focus on increasing the log P value. The inhibitory activity against prolyl oligopeptidase from pig brain was tested in vitro. The most promising ...