Benzanilides with spasmolytic activity: chemistry, pharmacology, and SAR.
The following study describes the synthesis of new benzanilide derivatives and their pharmacological investigation on smooth muscle preparations of guinea pigs. All compounds were synthesized in good yields and showed a spasmolytic activity without significant effect on vascular smooth muscles and heart muscle preparations. Moreover, further pharmacological investigations as well as in silico studies were performed to elucidate the mechanism of action. Compound 3 showed the most potent spasmolytic activity with an IC(50) of 3.25microM.
Brunhofer
Gerda
G
Department of Pharmaceutical Chemistry, University of Vienna, A-1090 Vienna, Althanstrasse 14, Austria.
Handler
Norbert
N
Leisser
Klaus
K
Studenik
Christian R
CR
Erker
Thomas
T
D000813:Anilides / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D004305:Dose-Response Relationship, Drug; D005260:Female; D006168:Guinea Pigs; D006325:Heart Atria / Q000187:drug effects; D007082:Ileum / Q000187:drug effects / Q000502:physiology; D020128:Inhibitory Concentration 50; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects* / Q000502:physiology; D010210:Papillary Muscles / Q000187:drug effects / Q000502:physiology; D000077185:Resveratrol; D013267:Stilbenes / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000813:Anilides; D013267:Stilbenes; C034595:benzanilide; D000077185:Resveratrol