Synthesis and structure-activity relationship of trimebutine derivatives.
Trimebutine derivatives were synthesized by utilizing alkylation or acylation of isonitriles and nitrile as a key step. The colonic contractile effects of these compounds were examined, and T-1815 was found to have strong colonic propulsive activity.
Sai
H
H
Lead Optimization Research Laboratory, Tanabe Seiyaku Co., Ltd., Osaka, Japan.
Ozaki
Y
Y
Hayashi
K
K
Onoda
Y
Y
Yamada
K
K
D000818:Animals; D003106:Colon / Q000187:drug effects; D005765:Gastrointestinal Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D005769:Gastrointestinal Motility / Q000187:drug effects; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship; D014287:Trimebutine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*
D005765:Gastrointestinal Agents; D014287:Trimebutine