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.
Baglin
I
I
Centre d'Etudes et de Recherche sur le Médicament de Normandie, Université de Caen, France.
Daveu
C
C
Lancelot
J C
JC
Bureau
R
R
Dauphin
F
F
Pfeiffer
B
B
Renard
P
P
Delagrange
P
P
Rault
S
S
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