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

Bioorganic and Medicinal Chemistry Letters

Volumn 13, Issue 24, 2003, Pages 4467-4471

  Breslin, Henry J ^a   Miskowski, Tamara A ^a   Kukla, Michael J ^a   De Winter, Hans L ^b   Somers, Maria V F ^b   Roevens, Peter W M ^b   Kavash, Robert W ^a  

^a LLC   (United States)

^b Johnson Johnson P   (Belgium)

Author keywords

[No Author keywords available]

Indexed keywords

CHOLECYSTOKININ OCTAPEPTIDE; ENZYME INHIBITOR; INDOLE DERIVATIVE; SERINE PROTEINASE; TRIPEPTIDYL PEPTIDASE II; UNCLASSIFIED DRUG;

ARTICLE; CONCENTRATION RESPONSE; DRUG ACTIVITY; DRUG POTENCY; DRUG STRUCTURE; ENZYME INHIBITION; IC 50; PHARMACOPHORE; PROTEIN DEGRADATION; STRUCTURE ACTIVITY RELATION;

EID: 0344741282     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2003.09.014     Document Type: Article

References (12)

1. Mokdad A.H., Serdula M.K., Dietz W.H., Bowman B.A., Marks J.S., Koplan J.P. JAMA. 282:1999;1519.
2. Must A., Spadano J., Coakley E.H., Field A.E., Colditz G., Dietz W.H. JAMA. 282:1999;1523.
3. Kordik C.P., Reitz A.B. J. Med. Chem. 42:1999;181.
4. Rose C., Vargas F., Facchinetti P., Bourgeat P., Bambal R.B., Bishop P.B., Chan S.M.T., Moore A.N.J., Ganellin C.R., Schwartz J.-C. Nature. 380:1996;403.
5. Breslin H.J., Miskowski T.A., Kukla M.J., Leister W.H., De Winter H.L., Gauthier D.A., Somers M.V.F., Peeters D.C.G., Roevens P.W.M. J. Med. Chem. 45:2002;5303.
6. Rose, C.; Vargas, F.; Bourgeat, P.; Schwartz, J.-C.; Bishop, P. B.; Bambal, R. B.; Ganellin, C. R.; Leblond, B.; Moore, A. N. J.; Chan, S.; Zhao, L. WO 9635805, 1996, CAN 136:72042.
7. Carpino L.A., Mansour E.-S.M.E., Sadat-Aalaee D. J. Org. Chem. 56:1991;2611.
8. Kashima C., Harada Y., Hosomi A. Heterocycles. 35:1993;433.
9. Gross K.M.B., Jun Y.M., Beak P. J. Org. Chem. 62:1997;7679.
10. Grimmett, M. R. In Imidazole and Benzimidazole Synthesis; Academic: San Diego, 1997; p 151.
11. Wasserman H.H., Vu C.B. Tetrahedron Lett. 31:1990;5205.
12. TPP II enzyme isolation and related determination of inhibitory activity are described in detail in ref 5.