First tricyclic oximino derivatives as 5-HT3 ligands

I Baglin; C Daveu; J C Lancelot; R Bureau; F Dauphin; B Pfeiffer; P Renard; P Delagrange; S Rault

doi:10.1016/s0960-894x(00)00691-0

First tricyclic oximino derivatives as 5-HT3 ligands

Bioorg Med Chem Lett. 2001 Feb 26;11(4):453-7. doi: 10.1016/s0960-894x(00)00691-0.

Authors

I Baglin¹, C Daveu, J C Lancelot, R Bureau, F Dauphin, B Pfeiffer, P Renard, P Delagrange, S Rault

Affiliation

¹ Centre d'Etudes et de Recherche sur le Médicament de Normandie, Université de Caen, France.

PMID: 11229746
DOI: 10.1016/s0960-894x(00)00691-0

Abstract

The design and synthesis of a new type of 5-HT3 ligand with subnanomolar affinity are described. The O-dialkylaminoethyloximinothienopyrrolizine structure was deduced from molecular modeling studies by replacement of an amidine moiety by an oximino one.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Colon / drug effects
Colon / physiology
Dose-Response Relationship, Drug
Guinea Pigs
In Vitro Techniques
Models, Molecular
Receptors, Serotonin / drug effects*
Receptors, Serotonin, 5-HT3
Serotonin Antagonists / chemical synthesis*
Serotonin Antagonists / pharmacology
Serotonin Receptor Agonists / chemical synthesis*
Serotonin Receptor Agonists / pharmacology
Structure-Activity Relationship

Substances

Receptors, Serotonin
Receptors, Serotonin, 5-HT3
Serotonin Antagonists
Serotonin Receptor Agonists