QSAR studies on 2-(benzyl)imidazolin analogs as h5-HT1D/1B serotonin receptor ligands

Authors
Prisinzano, T Law, H Slassi, A MaClean, N Demchyshyn, L Glennon, RA
Citation
T. Prisinzano et al., QSAR studies on 2-(benzyl)imidazolin analogs as h5-HT1D/1B serotonin receptor ligands, MED CHEM RE, 10(5), 2001, pp. 309-317
Citations number
22
Categorie Soggetti
Chemistry & Analysis
Journal title
MEDICINAL CHEMISTRY RESEARCH
ISSN journal
10542523 → ACNP
Volume
10
Issue
5
Year of publication
2001
Pages
309 - 317
Database
ISI
SICI code
1054-2523(2001)10:5<309:QSO2AA>2.0.ZU;2-7
Abstract
Human 5-HT1D/1B receptors are the likely therapeutic targets of several cli nically used migraine-abortive triptans such as sumatriptan. The present in vestigation, using several QSAR methods (e.g. CoMFA and Hansch analysis), a ttempts to better explain the structure-affinity relationships of 2-(benzyl )imidazolines and benzylimidazoline-related compounds for binding at h5-HT1 D receptors. It was found that lipophilicity at the 4-position of benzyl im idazolines correlates well both with h5-HT1D and h5-HT1B receptor affinity.