Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/4800
Title: α1-Adrenoceptor antagonists. 5. Pyridazinone-arylpiperazines. Probing the influence on affinity and selectivity of both ortho-Alkoxy groups at the arylpiperazine moiety and cyclic substituents at the pyridazinone nucleus
Authors: Betti, L.
Floridi, M.
Giannaccini, G.
Manetti, Fabrizio 
Strappaghetti, G.
Tafi, Andrea 
Botta, Maurizio 
Keywords: ANTIHYPERTENSIVE AGENTS; DERIVATIVES; QUINAZOLINES
Issue Date: 2003
Project: None 
Journal: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Abstract: 
Our previous work on pyridazinone-arylpiperazine derivatives suggested some structural features that a compound should have to show high affinity and good selectivity for alpha(1) adrenoceptors (AR) with respect to alpha(2)-AR. Accordingly, two classes of new alkoxyphenylpiperazinylheptylpyridazinones were designed and synthesized to evaluate the effect of the alkoxy substituent on affinity and selectivity. As expected, affinity increased with larger alkoxy groups. Affinity values are all comparable with that of the reference compound (prazosin), with the exception of compound 1c found 4.5-fold more active than prazosin
Description: 
19516
URI: http://hdl.handle.net/20.500.12779/4800
ISSN: 0960-894X
DOI: 10.1016/S0960-894X(02)00932-0
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