)-1,2,3,4-TETRAHYDRO[1]BENZOTHIENO[2,3-C]PYRIDINES - NOVEL OPTICALLY-ACTIVE COMPOUNDS WITH STRONG 5-HT(1A) RECEPTOR-BINDING ABILITY EXHIBITING ANTICONFLICT ACTIVITY AND LESSENING OF MEMORY IMPAIRMENT

Citation
H. Kawakubo et al., )-1,2,3,4-TETRAHYDRO[1]BENZOTHIENO[2,3-C]PYRIDINES - NOVEL OPTICALLY-ACTIVE COMPOUNDS WITH STRONG 5-HT(1A) RECEPTOR-BINDING ABILITY EXHIBITING ANTICONFLICT ACTIVITY AND LESSENING OF MEMORY IMPAIRMENT, Journal of medicinal chemistry, 36(23), 1993, pp. 3526-3532
Citations number
19
Categorie Soggetti
Chemistry Medicinal
ISSN journal
00222623
Volume
36
Issue
23
Year of publication
1993
Pages
3526 - 3532
Database
ISI
SICI code
0022-2623(1993)36:23<3526:)-NO>2.0.ZU;2-U
Abstract
R)-1,2,3,4-Tetrahydro[1]benzothieno[2,3-c]pyridine derivatives (60-114 ) were synthesized. The (R)-isomers have affinity for the 5-HT1A recep tor while the (S)-isomers have no such ability. The affinity of the (R )-isomers was discussed on the basis of structure-activity relationshi ps between the affinity-and hydrophobicity of the (R)-isomers. Compoun ds 71 and 107, which are representative derivative compounds, have ant iconflict activity and lessening of memory impairment. In particular, compound 107 cannot bind to receptors other than the 5-HT1A receptor, demonstrating that it is a unique compound with a different mechanism of action from that of conventional anxiolytics.