3-Benzo[b]furyl- and 3-benzo[b]thienylaminobutyric acids as GABAB ligands. Synthesis and structure - Activity relationship studies

European Journal of Medicinal Chemistry

Volumn 31, Issue 6, 1996, Pages 449-460

  Ansar, M ^a   Ebrik, S Al Akoum ^a   Mouhoub, R ^a   Berthelot, P ^a   Vaccher, C ^a   Vaccher, M P ^a   Flouquet, N ^a   Caignard, D H ^b   Renard, P ^b   Pirard, B ^c   Rettori, M C ^b   Evrard, G ^c   Durant, F ^c   Debaert, M ^a  

^a UNIV LILLE   (France)

^b ADIR   (France)

^c UNIVERSITY OF NAMUR   (Belgium)

Author keywords

3 heteroaromatic baclofen analogue; Benzo b furan; Benzo b thiophen; GABAB ligand; Structure activity relationship

Indexed keywords

3 BENZO[B]THIENYLAMINOBUTYRIC ACID DERIVATIVE; 4 AMINO 3 (BENZOFURAN 2 YL)BUTYRIC ACID; 4 AMINOBUTYRIC ACID B RECEPTOR; 4 AMINOBUTYRIC ACID DERIVATIVE; 4 AMINOBUTYRIC ACID RECEPTOR; UNCLASSIFIED DRUG;

ANIMAL TISSUE; ARTICLE; BRAIN SYNAPTOSOME; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG SYNTHESIS; LIGAND BINDING; NONHUMAN; RAT; RECEPTOR BINDING; STRUCTURE ACTIVITY RELATION;

EID: 0029994121     PISSN: 02235234     EISSN: None     Source Type: Journal    
DOI: 10.1016/0223-5234(96)85165-8     Document Type: Article

References (30)

1. GABA-Neurotransmitters. Pharmacochemical, Biochemical and Pharmacological Aspects (Krogsgaard-Larsen P, Scheel-Kruger J, Kofod H, eds) Munksgaard, Copenhagen (1979)
2. Möhler H (1992) Arzneim Forsch 42, 211-214
3. The GABA Receptors (Enna SJ, ed) Humana, Clifton, NJ (1983)
4. Bowery NG, Hill DR, Hudson AL et al (1980) Nature 283, 92-94
5. Bowery NG (1983) Classification of GABA Receptors. In: The GABA Receptor (Enna SJ, ed) Humana, Clifton, NJ, 177-213
6. Moratalla R, Bowery NG (1991) Neurochem Res 16, 309-314
7. Bowery NG (1993) Annu Rev Pharmacol Toxicol 33, 109-147
8. Kerr DIB, Ong J (1995) Pharmacol Ther 67, 2, 187-246
9. Krogsgaard-Larsen P (1981) J Med Chem 24, 1377-1383
10. Johnston GAR (1986) Multiplicity of GABA Receptors. In: Benzodiazepine/ GABA Receptors and Chloride Channels: Structural and Functional Properties (Olsen RW, Venter JC, eds) Alan R Liss, New York, 57-71
11. Drew CA, Johnston GAR (1992) J Neurochem 58, 1087-1092
12. Muller-Uri C, Singer EA, Fleischnacker W (1986) J Med Chem 29, 125-132
13. Kerr DIB, Ong J, Prager RH, Gynther BD, Curtis DR (1987) Brain Res 405, 150-154
14. Kerr DIB, Ong J, Johnston GAR, Abbenante J, Prager RH (1988) Neurosci Lett 92, 92-96
15. Berthelot P, Vaccher C, Musadad A, Flouquet N, Debaert M, Luyckx M (1987) J Med Chem 30, 743-746
16. Berthelot P, Vaccher C, Flouquet N, Debaert M, Luyckx M, Brunet C (1991) J Med Chem 34, 2557-2560
17. Thoer A, Denis G, Delmas M, Gaset A (1988) Synthetic Comm 18, 2095-2101
18. Duff JC (1941) J Chem Soc 547-550
19. Renz J (1947) Helv Chim Acta 124-139
20. Maillard J, Langlois M, Vo Van T et al (1983) Eur J Med Chem 18, 353-358
21. Hirota T, Fujita H, Sasaki K, Namba T (1986) Heterocycl Chem 23, 1715-1716
22. Dickinson RP, Iddon B, Sommerville RG (1973) Int J Sulfur Chem 8, 233-242
23. Flynn DL, Zelle RE, Grieco PA (1983) J Org Chem 48, 2424-2426
24. Enna SJ, Snyder SH (1975) Brain Res 100, 81-97
25. B antagonists: novel CNS-active compounds. In: Perspectives in Medicinal Chemistry (Testa B, Kyburz E, Fuhrer W, Giger R, eds) VCH, Basel, 259-272
26. Froestl W, Mickel SJ, Hall RG et al (1995) J Med Chem 38, 3297-3312
27. Froestl W, Mickel SJ, von Sprecher G et al (1995) J Med Chem 38, 3312-3331
28. Berthelot P, Vaccher C, Flouquet N et al (1991) Eur J Med Chem 26, 395-402
29. Pirard B, Evrard G, Norberg B et al (1993) Bull Soc Chim Belg 102, 639-643
30. Pirard B (1994) PhD thesis, Facultés Universitaires Notre-Dame-de-la-Paix, Namur, Belgique