First tricyclic oximino derivatives as 5-HT3 ligands.
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.
Centre d'Etudes et de Recherche sur le Médicament de Normandie, Université de Caen, France.
I
I
Baglin
C
C
Daveu
J C
JC
Lancelot
R
R
Bureau
F
F
Dauphin
B
B
Pfeiffer
P
P
Renard
P
P
Delagrange
S
S
Rault
D000818:Animals; D003106:Colon / Q000187:drug effects / Q000502:physiology; D004305:Dose-Response Relationship, Drug; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008958:Models, Molecular; D011985:Receptors, Serotonin / Q000187:drug effects*; D044406:Receptors, Serotonin, 5-HT3; D012702:Serotonin Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D017366:Serotonin Receptor Agonists / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D011985:Receptors, Serotonin; D044406:Receptors, Serotonin, 5-HT3; D012702:Serotonin Antagonists; D017366:Serotonin Receptor Agonists