Parallel solution- and solid-phase synthesis of spiropyrrolo-pyrroles as novel neurokinin receptor ligands

Bioorganic and Medicinal Chemistry Letters

Volumn 12, Issue 21, 2002, Pages 3073-3076

  Bleicher, Konrad H ^a   Wüthrich, Yves ^a   Adam, Geo ^a   Hoffmann, Torsten ^a   Sleight, Andrew J ^a  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

3,5 BIS(TRIFLUOROMETHYL)PHENYL; BENZENE DERIVATIVE; G PROTEIN COUPLED RECEPTOR; LIGAND; NEUROKININ 1 RECEPTOR; PYRROLE DERIVATIVE; SPIROPYRROLOPYRROLE; TACHYKININ RECEPTOR; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; CHEMICAL ANALYSIS; CHEMICAL REACTION; CONTROLLED STUDY; CYCLOADDITION; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TARGETING; HUMAN; HUMAN CELL; TECHNIQUE;

COMBINATORIAL CHEMISTRY TECHNIQUES; GTP-BINDING PROTEINS; INDICATORS AND REAGENTS; LIGANDS; PYRROLES; RECEPTORS, NEUROKININ-1; RECEPTORS, NEUROKININ-2; RECEPTORS, NEUROKININ-3; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0037020713     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(02)00659-5     Document Type: Article

References (11)

1. Beck-Sickinger A. Drug Discov. Today. 1:1996;502.
2. Leroy V., Mauser P., Gao Z., Peet N.P. Exp. Opin. Invest. Drugs. 9:1999;735.
3. Seward E.M., Swain C. Exp. Opin. Ther. Pat. 9:1999;571.
4. Bleicher, K. H.; Wüthrich, Y.; De Boni, M.; Kolczewski, S.; Hoffmann, T.; Sleight, A. J. Bioorg. Med. Chem. Lett. 2002, 12, 2519.
5. Mason J.S., Morize I., Menard P.R., Cheney D.L., Hulme C., Labaudiniere R.F. J. Med. Chem. 42:1999;3251.
6. Patchett A.A., Nargund R.P. Annu. Rep. Med. Chem. 35:2000;289.
7. Boehm H.-J., Boehringer M., Bur D., Gmuender H., Huber W., Klaus W., Kostrewa D., Kuehne H., Luebbers T., Meunier-Keller N., Mueller F. J. Med. Chem. 43:2000;2664.
8. Adam, G.; Dautzenberg, F.; Kolczewski, S.; Roever, S.; Wichmann, J. Eur. Pat. Appl. 963987 1999; Chem. Abstr. 1999, 132, 35624.
9. Reinscheid R.K., Nothacker H.P., Bourson A., Ardati A., Henningsen R.A., Bunzow J.R., Grandy D.K., Langen H., Monsma F.J. Jr., Civelli O. Science. 270:1995;792.
10. Tsuge O., Kanemasa S., Ohe M., Yorozu K., Takenaka S., Ueno K. Bull. Chem. Soc. Jpn. 60:1987;4067.
11. 3H] substance P. Displacement curves were determined with at least seven concentrations of the compound.