2024-03-29T15:52:40Zhttp://digital.csic.es/dspace-oai/requestoai:digital.csic.es:10261/446322019-03-04T08:29:07Zcom_10261_81com_10261_5col_10261_334
2012-01-24T10:36:54Z
urn:hdl:10261/44632
New aromatic iminoimidazolidine derivatives as alpha(1)-adrenoceptor antagonists: A novel synthetic approach and pharmacological activity
Dardonville, Christophe
Goya, Pilar
Rozas, Isabel
Alsasua, Ángela
Martín, M. Isabel
The design, synthesis and a1-adrenoceptor antagonism of a series of bis-imidazoline (1a, 2a, 3a and 4a) and bis-guanidine
(1b, 2b, 3b and 4b) diphenyl derivatives are reported. All of these compounds ful®l the conditions of the most recent pharmaco-
phore proposed for a1-adrenoceptors and found in the literature. Besides, a novel synthetic approach to the preparation of 2-(aryl-
imino)imidazolidine derivatives is described. All the tested compounds, except the bis-guanidinium derivative 3b, inhibit the
contractile responses induced by noradrenaline in aortic rings of rat and rabbit in a dose-dependent manner. Our results indicate
that, even though some discrepancies are observed in terms of the a1 subtype targeted by this new family of compounds, they show
an interesting pro®le as antagonists of a1-adrenoceptors and a new prototype, compound 1a, has been found deserving further
development
2012-01-24T10:36:54Z
2012-01-24T10:36:54Z
2000-07
artículo
Bioorganic and Medicinal Chemistry 8 (7) : 1567-1577 (2000)
0968-0896
http://hdl.handle.net/10261/44632
eng
http://144.206.159.178/FT/115/19407/346689.pdf
closedAccess
Pergamon Press