Synthesis and choleretic activity of 3-[2-(3-R', 4-R'', 5-R'''-benzyl)-5-R-benzimidazol-1-yl]-butanoic acids.
On the ground of the evidentiated choleretic activity of 3-[2-benzylbenzimidazol-1-yl]butanoic acid, 28 new acids were prepared in order to evaluate the influence of suitable substitutions in either C5 of heteroring or C3', C4', C5' of benzyl group in position 2 on the choleretic activity. Pharmacological results after i.v. administration of 0.5 mmol/Kg in rats confirmed a general high choleretic activity that in eleven cases showed during the first 4 hours an increase of bile volume higher than 80%, that is superior to that produced by dehydrocholic acid. Only in a few cases the bile volume increase was less than 37% of basal value.
Grella
G
G
Istituto di Chimica Farmaceutica e Tossicologica, Università di Sassari.
Paglietti
G
G
Sparatore
F
F
Satta
M
M
Manca
P
P
Peana
A
A
D000818:Animals; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D001646:Bile / Q000187:drug effects / Q000378:metabolism; D001647:Bile Acids and Salts / Q000378:metabolism; D002087:Butyrates / Q000138:chemical synthesis* / Q000494:pharmacology; D002756:Cholagogues and Choleretics / Q000138:chemical synthesis* / Q000494:pharmacology; D003685:Dehydrocholic Acid / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains
D001562:Benzimidazoles; D001647:Bile Acids and Salts; D002087:Butyrates; D002756:Cholagogues and Choleretics; D003685:Dehydrocholic Acid