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Synthesis and choleretic activity of 3-[2-(3-R', 4-R'', 5-R'''-benzyl)-5-R-benzimidazol-1-yl]-butanoic acids

Grella, Giuseppe Enrico and Paglietti, Giuseppe and Sparatore, Fabio and Satta, Margherita and Manca, Paola and Peana, Alessandra Tiziana (1992) Synthesis and choleretic activity of 3-[2-(3-R', 4-R'', 5-R'''-benzyl)-5-R-benzimidazol-1-yl]-butanoic acids. Il Farmaco, Vol. 47 (1), p. 21-35. ISSN 0014-827X. Article.

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Abstract

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.

Item Type:Article
ID Code:8665
Status:Published
Refereed:Yes
Uncontrolled Keywords:Choleretic activity, butanoic acid, bile volume
Subjects:Area 05 - Scienze biologiche > BIO/14 Farmacologia
Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01 Dipartimenti > Farmaco, chimico, tossicologico
001 Università di Sassari > 01 Dipartimenti > Scienze del farmaco
Publisher:Società chimica italiana
ISSN:0014-827X
Publisher Policy:Depositato per gentile concessione dell'Editore
Additional Information:Part of this work was presented as poster communication at 6th National Meeting of the Division of Medicinal Chemistry of the Societa Chimica Italiana, Alghero, 14-18 October 1986.
Deposited On:21 Feb 2013 12:29

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