alpha(1)-Adrenoceptor antagonists. Rational design, synthesis and biological evaluation of new trazodone-like compounds.
A rational design approach has been applied to synthesize a novel class of compounds with affinity for alpha(1) adrenergic receptors (AR). Molecular structures are characterized by a benzimidazolylpyridazinone or an imidazolylpyridazinone moiety, an original fragment in the field of the arylpiperazine compounds with alpha(1)-AR blocking properties. A 1.1 nM affinity toward alpha(1)-AR was found for compound 3, the most active of this series.
Betti
Laura
L
Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy.
Botta
Maurizio
M
Corelli
Federico
F
Floridi
Monia
M
Fossa
Paola
P
Giannaccini
Gino
G
Manetti
Fabrizio
F
Strappaghetti
Giovannella
G
Corsano
Stefano
S
D058668:Adrenergic alpha-1 Receptor Antagonists; D000478:Alkylation; D000818:Animals; D018687:Antidepressive Agents, Second-Generation / Q000138:chemical synthesis* / Q000494:pharmacology; D001667:Binding, Competitive / Q000187:drug effects; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D006827:Hydantoins / Q000737:chemistry; D008958:Models, Molecular; D011869:Radioligand Assay; D051381:Rats; D013329:Structure-Activity Relationship; D014196:Trazodone / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology
D058668:Adrenergic alpha-1 Receptor Antagonists; D018687:Antidepressive Agents, Second-Generation; D006827:Hydantoins; D014196:Trazodone