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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 |
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| Authors: | Breslin Henry J Miskowski Tamara A Kukla Michael J De Winter Hans L Somers Maria V F Roevens Peter W M Kavash Robert W |
| Affiliation: | a Johnson & Johnson Pharmaceutical Research & Development, L.L.C., Welsh and McKean Roads, PO Box 776, Spring House, PA 19477-0776, USA b Johnson & Johnson Pharmaceutical Research & Development, L.L.C., Turnhoutseweg 30, B-2340, Beerse, Belgium |
| 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 4-11 nM). |
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