1-phenyl-4(1H)-quinazolinones and 2,3-dihydro-1-phenyl-4(1H)-quinazolinones as potential cholecystokinin receptor ligands

Journal of Heterocyclic Chemistry

Volumn 33, Issue 4, 1996, Pages 1163-1170

  Pentassuglia, Giorgio ^a   Bertani, Barbara ^a   Donati, Daniele ^a   Ursini, Antonella ^a  

^a GSK   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

CHOLECYSTOKININ A RECEPTOR; CHOLECYSTOKININ RECEPTOR BLOCKING AGENT; QUINAZOLINE DERIVATIVE;

ANIMAL CELL; ANIMAL TISSUE; ARTICLE; BRAIN CORTEX; CONTROLLED STUDY; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; GUINEA PIG; NONHUMAN; PANCREAS; REACTION ANALYSIS; STRUCTURE ACTIVITY RELATION;

EID: 0029821699     PISSN: 0022152X     EISSN: None     Source Type: Journal    
DOI: 10.1002/jhet.5570330427     Document Type: Article

References (17)

1. C. A. Baile, C. L. McLaughlin, and M. A. Della-Ferra, Physiol. Rev., 66, 172 (1986).
2. C. A. Altar, Prog. Neuro-Psychopharmacol. Sci., 13, 381 (1989).
3. J. M. Kerwin, Drugs Future, 16, 1111 (1991).
4. H. Finch, D. G. Trist, G. Tarzia, and A. Feriani, Glaxo S.p.A., WO93/14074 (1993); Chem. Abstr., 120, 134541 (1994).
5. H. Finch, D. G. Trist, G. Tarzia, and A. Feriani, Glaxo S.p.A., WO93/14074 (1993); Chem. Abstr., 120, 134541 (1994).
6. D. G. Trist, G. Pentassuglia, M. E. Tranquillini, and A. Ursini, Glaxo S.p.A., WO93/14075 (1993); Chem. Abstr, 120, 164241 (1994).
7. D. G. Trist, G. Pentassuglia, M. E. Tranquillini, and A. Ursini, Glaxo S.p.A., WO93/14075 (1993); Chem. Abstr, 120, 164241 (1994).
8. G. Curotto, D. Donati, G. Finizia, and A. Ursini, Tetrahedron: Asimmetry, 6, 849 (1995).
9. B. E. Evans, M. G. Bock, K. E. Rittle, R. M. DiPardo, W. L. Whitter, D. F. Veber, P. S. Anderson, and R. M. Freidinger, Proc. Natl. Acad Sci. U.S.A., 83, 4918 (1986).
10. M. J. Yu, K. J.Thrasher, J. R. McCowan, N. R.Mason, and L. G. Mendelsohn, J. Med. Chem., 34, 1505 (1991).
11. J. J. Howbert, K. L. Lobb, T. C. Britton, N. R. Mason, and R. F. Bruns, Bioorg. Med. Chem. Letters, 3, 875 (1993).
12. B. K. Trivedi, Current Med. Chem., 1, 313 (1994).
13. Systematic conformational searches were carried out on L-365-260 and compound 1. The resulting conformations were minimised applying BFGS and filtered using a 4 Kcal/mol energy window. Finally, representative conformers for each structure were superimposed, selecting the centroids of the aromatic rings as reference points. Only the conformations below 0.5 rms deviation were accepted.
14. K. Ozaki, Y. Yamada, and T. Oine, Chem. Pharm. Bull., 31, 2234 (1983).
15. A. Van Dijk, J. G. Richards, A. Trzeciak, D. Gillessen, and H. Moehler, J. Neurosci., 4, 1021 (1984).
16. R. B. Innis and S. H. Snyder, Proc. Natl. Acad. Sci. U.S.A., 77, 6917 (1980).
17. S. Raucher, B. L. Bray, and R. L. Lawrence, J. Am. Chem. Soc., 109, 442 (1987).