Novel 2,5-disubstituted-1H-pyrroles with high affinity for the dopamine D3 receptor: N-benzyl modifications

Bioorganic and Medicinal Chemistry Letters

Volumn 7, Issue 3, 1997, Pages 327-330

  Boyfield, Izzy ^a   Coldwell, Martyn C ^a   Hadley, Michael S ^a   Healy, Maureen A M ^a   Johnson, Christopher N ^a   Nash, David J ^a   Riley, Graham J ^a   Scott, Emma E ^a   Smith, Stephen A ^a   Stemp, Geoffrey ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

DOPAMINE 2 RECEPTOR; DOPAMINE 3 RECEPTOR; PYRROLE DERIVATIVE;

ARTICLE; BRAIN; CONTROLLED STUDY; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; ENANTIOMER; HUMAN; HUMAN CELL; MOLECULAR CLONING; NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY; STRUCTURE ACTIVITY RELATION;

EID: 0031552093     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(96)00621-X     Document Type: Article

References (6)

1. 1. Grandy, D. K.; Marchionni, M. A.; Makam, H.; Stofko, R. E.; Alfano, M.; Frothingham, L.; Fischer, J. B.; Burke-Howie, K. J.; Bunzow, J. R.; Server, A. C.; Civelli, O. Proc. Nat. Acad. Sci. 1989, 86, 9762-9766.
2. 2. Sokoloff, P.; Giros, B.; Martres, M-P.; Bouthenet, M-L.; Schwartz, J-C. Nature. 1990, 347, 146-151.
3. 3. Van Tol, H. H. M.; Bunzow, J. R.; Guan, H-C.; Sunahara, R. K.; Seeman, P.; Niznik, H. B.; Civelli, O. Nature. 1991, 350, 610-614.
4. 4. Bolton, D.; Boyfield, I.; Coldwell, M. C.; Hadley, M. S.; Healy, M. A.; Johnson, C. N.; Markwell, R. E.; Nash, D. J.; Riley, G. J.; Stemp, G.; Wadsworth, H. BioMed. Chem. Letts. 1996, 6, 1233-1236.
5. 5. van Wijngaarden, I.; Kruse, C. G.; van Hes, R.; van der Heyden, J. A. M.; Tulp, M. T. M. J. Med. Chem. 1987, 30, 2099-2104.
6. 1H (mixture of protomers): δ 1.30 (m, 6H), 2.30-2.65 (m, 2H), 2.70-3.20 (m, 6H), 4.10-4.55 (m, 2H), 4,20 (s, 3H), 4.95 and 5.05 (2 x t, 1H), 6.30 and 6.35 (2 x m, 1H), 6.55 (m, 1H), 7.10 (d, 1H), 7.30 (m, 3H), 7.70 and 7.85 (2 x dd, 1H), 8.15 (m, 1H), 11.70 and 11.95 (2 x brs, 1H), 12.30 and 12.55 (2 x br s, 1H).