Tripeptidyl-peptidase II (TPP II) inhibitory activity of (S)-2, 3-dihydro-2-(1H-imidazol-2-yl)-1H-indoles, a systematic SAR evaluation. Part 2

…, TA Miskowski, MJ Kukla, HL De Winter…

Index: Breslin, Henry J.; Miskowski, Tamara A.; Kukla, Michael J.; De Winter, Hans L.; Somers, Maria V. F.; Roevens, Peter W. M.; Kavash, Robert W. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 24 p. 4467 - 4471

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Citation Number: 22

Abstract

We have systematically explored the structure–activity relationship (SAR) for a series of compounds 2 as inhibitors of tripeptidyl-peptidase II (TPP II), a serine protease responsible for the degradation of cholecystokinin-8 (CCK-8). This SAR evaluation of the core structure 2 suggest a fairly restrictive pharmacophore for such related structures, but has yielded a limited set of compounds (2b, 2c, 2d, 2s, and 2t) with potent TPP II inhibitory activity (IC50 ...