Automated parallel synthesis of a tetrahydroisoquinolin-based library: Potential prolyl endopeptidase inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 9, Issue 3, 1999, Pages 437-442

  Vendeville, Sandrine ^a   Bourel, Line ^a   Davioud Charvet, Elisabeth ^a   Grellier, Philippe ^b   Déprez, Benoît ^c   Sergheraert, Christian ^a  

^a INSTITUT PASTEUR DE LILLE   (France)

^b MUSÉUM NATIONAL D'HISTOIRE NATURELLE   (France)

^c CEREP   (France)

Author keywords

[No Author keywords available]

Indexed keywords

AMINE; CARBOXYLIC ACID; PROLYL ENDOPEPTIDASE INHIBITOR; PYRROLIDINE DERIVATIVE; TETRAHYDROISOQUINOLINE DERIVATIVE;

ARTICLE; DRUG ACTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME SPECIFICITY; REACTION ANALYSIS; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS; TRYPANOSOMA CRUZI;

ISOQUINOLINES; SERINE ENDOPEPTIDASES; SERINE PROTEINASE INHIBITORS; SUBSTRATE SPECIFICITY;

TRYPANOSOMA; TRYPANOSOMA CRUZI;

EID: 0033535121     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(99)00003-7     Document Type: Article

References (16)

1. Déprez, B.; Williard, X.; Bourel, L.; Coste, H.; Hyafil, F.; Tartar, A. J. Am. Chem. Soc. 1995, 117, 5405.
2. Santana, J. M.; Grellier, P; Schrevel, J.; Teixeira, A. Biochem. J. 1997, 324, 129.
3. Vendeville, S.; Buisine, E.; Williard, X.; J. M.; Schrevel, J.; Grellier, P.; Santana, J. M.; Sergheraert, C. Chem. Pharm. Bull. 1998, in press.
4. Unpublished results.
5. Polgar, L. Methods in Enzymology 1994, 244, 14, 188.
6. Fülop, V.; Böcskei, Z.; Polgar, L. Cell 1998, 94, 161.
7. Higuchi, N.; Saito, N.; Hashimoto, M.; Hukami, H.; Tanaka, T. Japan. Patent. 1988, 201877, Chem. Abstr. 1988, 108, 75852m.
8. Yoshimoto, T.; Tsuru, D.; Yamamoto, N.; Ikesawa, R.; Furukawa, S. Agric. Biol. Chem. 1991, 55, 37.
9. Saito, M.; Hashimoto, M.; Kawaguchi, N.; Shibata, H.; Fukami, H.; Tanaka, T.; Higuchi, N. J. Enzyme Inhibition. 1991, 5, 51.
10. min + 5 kcal/mol.
11. Goodman, M.; Chorev, M. Acc. Chem. Res. 1979, 12, 1.
12. Tsuru, D.; Yoshimoto, T.; Koriyama, N.; Furukawa, S. J. Biochem. 1988, 104, 580.
13. Poitevin, B.; Benoist, A.; Rémond, G.; Hervé, Y.; Vincent, M.; Lepagnol, J.; De Nanteuil, G. J. Med. Chem. 1996, 39, 2379.
14. 50 value, which was defined as the concentration of the test compound that resulted in 50% inhibition of the fluorescence with respect to the DMSO control.
15. 2, 80% acetonitrile.
16. Kolosko, N.; Bakker, A.V.; Faraci, W.S.; Nagel, A.A. Drug Design and Discovery 1994, 11, 61.