Novel carbazole derivatives as NPY Y1 antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 17, Issue 4, 2007, Pages 1043-1046

  Leslie, Colin P ^a   Fabio, Romano Di ^a   Bonetti, Francesca ^a   Borriello, Manuela ^a   Braggio, Simone ^a   Forno, Giovanna Dal ^a   Donati, Daniele ^a   Falchi, Alessandro ^a   Ghirlanda, Damiano ^a   Giovannini, Riccardo ^a   Pavone, Francesca ^a   Pecunioso, Angelo ^a   Pentassuglia, Giorgio ^a   Pizzi, Domenica A ^a   Rumboldt, Giovanna ^a   Stasi, Luigi ^a  

^a GSK   (Italy)

Author keywords

CNS; Neuropeptide Y; NPY Y1 antagonist; Obesity

Indexed keywords

CARBAZOLE DERIVATIVE; METHYLCELLULOSE; NEUROPEPTIDE Y RECEPTOR ANTAGONIST; NEUROPEPTIDE Y1 RECEPTOR;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BRAIN; CHEMICAL REACTION; DRUG BIOAVAILABILITY; DRUG PENETRATION; DRUG STRUCTURE; DRUG SYNTHESIS; MALE; NONHUMAN; PHYSICAL CHEMISTRY; RAT; STRUCTURE ACTIVITY RELATION;

ANIMALS; BIOLOGICAL AVAILABILITY; BRAIN; CARBAZOLES; CHEMISTRY, PHYSICAL; CHO CELLS; CRICETINAE; CRICETULUS; HALF-LIFE; INDICATORS AND REAGENTS; MALE; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, NEUROPEPTIDE Y; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 33846625862     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.11.034     Document Type: Article

References (14)

1. Tatemoto K., Carlquist M., and Mutt V. Nature 296 (1982) 659
2. O'Donohue T.L., Chronwall B.M., Pruss R.M., Mezey E., Kiss J.Z., Eiden L.E., Massari J., Tessel E., Pickel V.M., Dimaggio D.A., Hotchkiss A.J., Crowly W.R., and Zukowska-Grojec Z. Peptides 6 (1985) 755
3. Tatemoto K., Mann M.J., and Shimizu M. Proc. Natl. Acad. Sci. U.S.A 89 (1992) 1174
4. Stanley B.G., and Leibowitz S.F. Proc. Natl. Acad. Sci. U.S.A 82 (1985) 3940
5. Boublik J.H., Scott N.A., Brown M.R., and Rivier J.E. J. Med. Chem. 32 (1989) 597
6. Heilig M., and Widerlov E. Acta Psychiatr. Scand. 82 (1990) 95
7. Rudolf K., Eberlein W., Engel W., Wieland H.A., Willim K.D., Entzeroth M., Wienem W., Beck-Sickinger A.G., and Doods H.N. Eur. J. Pharmacol. 271 (1994) R11
8. Serradeil-Le Gal C., Valette G., Rouby P.-E., Pellet A., Oury-Donat F., Brossard G., Lepsy L., Marty E., Neliat G., Conite P., Maffrand J.-P., and Le Fur G. FEBS Lett. 362 (1995) 192
9. Wright J., Bolton G., Creswell M., Downing D., Georgic L., Heffner T., Hodges J., MacKenzie R., and Wise L. Bioorg. Med. Chem. Lett. 6 (1996) 1809
10. Hipskind P.A., Lodd K.L., Nixon J.A., Britton T.C., Bruns R.F., Catlow J., Dieckman-McGinty D.K., Gackenheimer S.L., Gitter B.D., Iyengar S., Schober D.A., Simmons R.M.A., Swanson S., Zarrinmayeh H., Zimmerman D.M., and Gehlert D.R. J. Med. Chem. 40 (1997) 3712
11. Kanatani A., Hata M., Mashiko S., Ishihara A., Okamoto O., Haga Y., Ohe T., Kanno T., Murai N., Ishii Y., Fukuroda T., Fukami T., and Ihara M. Mol. Pharmacol. 59 (2001) 501
12. Di Fabio R., Giovannini R., Bertani B., Borriello M., Bozzoli A., Donati D., Falchi A., Ghirlanda D., Leslie C.P., Pecunioso A., Rumboldt G., and Spada S. Bioorg. Med. Chem. Lett. 16 (2006) 1749
13. Unpublished results, GSK.
14. a unit drop compared to the non-alkylated amines (for example, see Gillaspy, M. L.; Lefker, B. A.; Hada, W. A.; Hoover, D. J. Tetrahedron Lett. 1995, 41, 7399).