28657-38-7Relevant academic research and scientific papers
Aminopyridazines as acetylcholinesterase inhibitors
Contreras, Jean-Marie,Rival, Yveline M.,Chayer, Said,Bourguignon, Jean-Jacques,Wermuth, Camille G.
, p. 730 - 741 (2007/10/03)
Following the discovery of the weak, competitive and reversible acetylcholinesterase (AChE)-inhibiting activity of minaprine (3c) (IC50 = 85 μM on homogenized rat striatum AChE), a series of 3-amino-6- phenylpyridazines was synthesized and tested for inhibition of AChE. A classical structure-activity relationship exploration suggested that, in comparison to minaprine, the critical elements for high AChE inhibition are as follows: (i) presence of a central pyridazine ring, (ii) necessity of a lipophilic cationic head, (iii) change from a 2- to a 4-5-carbon units distance between the pyridazine ring and the cationic head. Among all the derivatives investigated, 3-[2-(1-benzylpiperidin-4-yl)ethylamino]-6- phenylpyridazine (3y), which shows an IC50 of 0.12 μM on purified AChE (electric eel), was found to be one of the most potent anti-AChE inhibitors, representing a 5000-fold increase in potency compared to minaprine.
3-Aminopyridazine derivatives with atypical antidepressant, serotonergic, and dopaminergic activities
Wermuth,Schlewer,Bourguignon,Maghioros,Bouchet,Moire,Kan,Worms,Biziere
, p. 528 - 537 (2007/10/02)
Minaprine [3[(β-morpholinoethyl)amino]4-methyl-6-phenylpyridazine dihydrochloride] is active in most animal models of depression and exhibits in vivo a dual dopaminomimetic and serotoninomimetic activity profile. In an attempt to dissociate these two effe
Substituted phenyl-1,2,4-triazolo[2,3-b]pyridazin-3(2H)ones as anti-asthma agents
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, (2008/06/13)
Substituted phenyl-1,2,4-triazolo[4,3-b]pyridazin-3(2H)-ones, useful as anti-asthma agents.
Method for treating anxiety in mammals
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, (2008/06/13)
This disclosure describes compositions of matter useful as anxiolytic agents and the method of meliorating anxiety in mammals therewith; the active ingredients of said compositions of matter being certain substituted 6-phenyl-1,2,4-triazolo[4,3-b]pyridazines or the pharmacologically acceptable acid-addition salts thereof.
6-Phenyl-1,2,4-triazolo[4,3-b]pyridazine hypotensive agents
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, (2008/06/13)
This disclosure describes novel substituted 6-phenyl-1,2,4-triazolo[4,3-b]pyridazines useful as hypotensive agents.
