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New aromatic iminoimidazolidine derivatives as alpha(1)-adrenoceptor antagonists: A novel synthetic approach and pharmacological activity

AuthorsDardonville, Christophe ; Goya, Pilar ; Rozas, Isabel; Alsasua, Ángela; Martín, M. Isabel
Issue DateJul-2000
PublisherPergamon Press
CitationBioorganic and Medicinal Chemistry 8 (7) : 1567-1577 (2000)
AbstractThe 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
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