Morphan based substance P antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 6, Issue 1, 1996, Pages 13-16

  Cocker, J D ^a   Chan, Chuen ^a   Davies, H G ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

2 AZABICYCLO[3.3.1]NONANE DERIVATIVE; 3 (2 METHOXYBENZYLAMINO) 2 PHENYLPIPERIDINE; BICYCLO[3.3.1]NONANE DERIVATIVE; NEUROKININ 1 RECEPTOR; SUBSTANCE P ANTAGONIST; UNCLASSIFIED DRUG;

ARTICLE; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; HUMAN CELL; NUCLEAR MAGNETIC RESONANCE; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

EID: 0343526174     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/0960-894X(95)00552-5     Document Type: Article

References (12)

1. Lotz, M.; Carson, D.A.; Vaughan, J.H. Science 1987, 235.
2. Lowe, J.A.; Snider, R.M. Annual Reports in Medicinal Chemistry 1993, 28, 99-107.
3. Moskowitz, M.A. Trends Pharmacol. Sci. 1992, 13, 307-311.
4. Otsuka, M.; Yanigasaga, M. J. Physiol. (London) 1988, 395, 255-270.
5. Desai, M.C. Exp. Opin. Ther. Patents 1994, 4 (4), 315-321.
6. Desai, M.C.; Thadeio, P.F.; Lefkowitz, S.L. Tetrahedron Lett. 1993, 34, 5831-5834.
7. Bountra, C.; Bunce, K.; Dale, T.; Gardner, C.; Jordan, C.; Twissell D.; Ward, P. Eur. J. Pharmacol., 1993, 249, R3-R4.
8. Tattersall, F.D.; Rycroft, W.; Hargreaves, R.J.; Hill, R.G. Eur. J. Pharmacol. 1993, 250, R5-R6.
9. Piperidine ring constrained analogues of CP 99,994 have been synthesised but no biological activities have been reported: Desai, M.C.; Lefkowitz, S.L. Tetrahedron Lett. 1994, 35, 4701-4704. For cyclic constrained analogues of the side-chain in CP 99,994 see: Desai, M.C.; Vincent, L.A.; Rizzi, J.P. J. Med. Chem., 1994, 37, 4263-4266.
10. Piperidine ring constrained analogues of CP 99,994 have been synthesised but no biological activities have been reported: Desai, M.C.; Lefkowitz, S.L. Tetrahedron Lett. 1994, 35, 4701-4704. For cyclic constrained analogues of the side-chain in CP 99,994 see: Desai, M.C.; Vincent, L.A.; Rizzi, J.P. J. Med. Chem., 1994, 37, 4263-4266.
11. 2O) δ 7.55-7.45 (m, 5H), 7.25 (m, 3H), 7.0 - 6.92 (m, 2H) 5.70 (br. s, 1H), 4.35 (d, J=12, 1H), 4.14 (d, J=12, 1H), 4.09 (s, 1H), 3.63 (s, 3H), 3.52 (m, 1H), 3.06 (m, 1H), 2.13 (d, J=19, 1H), 2.69 (d, J=19, 1H), 2.18 (m, 1H), 2.01 (m, 1H), 1.84 (s, 3H).
12. i values) were determined.