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  • Title: 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.
    Author: Breslin HJ, Miskowski TA, Kukla MJ, De Winter HL, Somers MV, Roevens PW, Kavash RW.
    Journal: Bioorg Med Chem Lett; 2003 Dec 15; 13(24):4467-71. PubMed ID: 14643348.
    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 (IC(50) 4-11 nM).
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