On the bioactive conformation of the GABA uptake inhibitor SK and F 89976-A

Bioorganic and Medicinal Chemistry Letters

Volumn 6, Issue 13, 1996, Pages 1535-1540

  Dhar, T G Murali ^a,b   Nakanishi, Hiroshi ^a,c   Borden, Laurence A ^a,d   Gluchowski, Charles ^a  

^a H LUNDBECK A S   (Denmark)

^b DUPONT COMPANY   (United States)

^c Molecumetics Ltd   (United States)

^d Trophix Pharmaceuticals Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 (4,4 DIPHENYL 3 BUTENYL)NIPECOTIC ACID; 4 AMINOBUTYRIC ACID; 4 AMINOBUTYRIC ACID RECEPTOR BLOCKING AGENT;

4 AMINOBUTYRIC ACID UPTAKE; ANXIETY; ARTICLE; DRUG CONFORMATION; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; EPILEPSY;

EID: 0030576311     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(96)00268-5     Document Type: Article

References (14)

1. 4. Kanner, B. I.; Schuldiner, S. Critical Review of Biochemistry; CRC: Boca Raton, 1987; Vol. 22, pp 1-38.
2. 5. Krogsgaard-Larsen, P.; Falch, E.; Larsson, E. M.; Schousboe, A. Epilepsy Res. 1987, 1, 77.
3. 6. Ali, F. E.; Bondinell, W. E.; Dandridge, P. A.; Frazee, J. S.; Garvey, E.; Girad, G. R.; Kaiser, C.; Ku, T. W.; Lafferty, J. J.; Moosanmy, G. I.; Oh, H. J.; Rush, J. A.; Setler, P. E.; Stringer, O. D.; Venslavsky, J. W.; Volpe, B. W.; Yunger, L. M.; Zirkle, C. L. J. Med. Chem. 1985, 28, 653.
4. 7. Suzdak, P. D. Drugs of the Future. 1993, 18, 1129, and references cited therein.
5. 8. Mengel, H. Epilepsia (suppl. 5). 1994, 35, 581.
6. 9. Smith, K. E.; Gustafson, E. L.; Borden, L. A.; Dhar, T. G. M.; Durkin, M. M.; Vaysse, P.J-J.; Branchek, T. A.; Gluchowski, C.; Weinshank, R. L. GABA Symposium 95, July 7-10, 1995, Kyoto Japan.
7. 10. Pavia, M. R.; Lobbestael, S. J.; Nugiel, D.; Mayhugh, D. R.; Gregor, V. E.; Taylor, C. P.; Schwarz, R. D.; Brahce, L.; Vartanian, M. G. J. Med. Chem. 1992, 35, 4238.
8. 11a. Borden, L. A.; Dhar, T. G. M.; Smith, K. E.; Weinshank, R. L.; Branchek, T. A.; Gluchowski, C. Eur. J. Pharm. 1994, 269, 219.
9. 11b. Dhar, T. G. M.; Borden, L. A.; Tyagarajan, S.; Smith, K. E.; Branchek, T. A.; Weinshank, R. L.; Gluchowski, C. J. Med. Chem. 1994, 37, 2334.
10. 12. N'Goka, V.; Schlewer, G.; Linget, J. M.; Chambon, J. P.; Wermuth, C. G. J. Med. Chem. 1991, 34, 2547.
11. 13. Goka et al. used the SYBYL program as part of their effort to generate the general pharmacophore model for GABA uptake inhibitors (ref 12).
12. 14. Dhar, T. G. M.; Gluchowski, C. Tetrahedron. Lett. 1994, 35, 989.
13. α- radiation. The structure was solved using "Direct Methods" techniques with the Siemens SHELXTL-PC software package as modified at Crystalytics Company. The refined fractional atomic coordinates, the bond lengths, bond angles, the hydrogen atom coordinates and thermal parameters have been deposited at the Cambridge Crystallographic Data Center (CCDC).
14. 16. Brehm, L.; Krogsgaard-Larsen, P.; Johnston, G. A. R.; Schaumburg, K. Acta. Chem. Scand. 1976, B30, 542.