1722-11-8Relevant articles and documents
Synthesis and Biological Evaluation of 2-substituted-6-(morpholinyl/piperidinyl)pyridazin-3(2H)-ones as Potent and Safer Anti-inflammatory and Analgesic Agents
Singh, Jyoti,Sharma, Deepika,Bansal, Ranju
, p. 2935 - 2945 (2017)
A series of 2-substituted-6-(morpholinyl/piperidinyl)pyridazin-3(2H)-ones was synthesized and the structures were established using various spectroscopic techniques. The target compounds were screened for anti-inflammatory and analgesic activities at 20 and 40?mg/kg. The safety of the synthesized derivatives was evaluated by assessing anti-platelet activity and ulcer index. The obtained pharmacological data revealed that 6-morpholinyl derivatives 4a–12a were found to be somewhat more potent than 6-piperidinyl derivatives 4b–6b. The 6-morpholinyl substituted pyridazinone 12a exhibited maximum anti-inflammatory and analgesic activities. Homoveratrylamine substituted compounds 6a and 6b emerged as promising leads in both the series with good anti-inflammatory and analgesic activities without any ulcerogenicity. Anti-platelet activity results of the compounds of both the series showed significantly low bleeding time in comparison with standard drug aspirin indicating the cardiovascular safety of new pyridazinones.
Selective mono-amination of dichlorodiazines
Sengmany, Stéphane,Lebre, Julie,Le Gall, Ewan,Léonel, Eric
, p. 4859 - 4867 (2015/08/03)
A mild, easy-to-perform, and versatile method for the formation of aminochlorodiazines from reaction of several types of dichlorodiazines (i.e., pyridazines, pyrimidines, and pyrazines) with primary or secondary amines in ethanol in the presence of trieth
Structure-activity relationship studies of SEN12333 analogues: Determination of the optimal requirements for binding affinities at α7 nAChRs through incorporation of known structural motifs
Beinat, Corinne,Reekie, Tristan,Banister, Samuel D.,O'Brien-Brown, James,Xie, Teresa,Olson, Thao T.,Xiao, Yingxian,Harvey, Andrew,O'Connor, Susan,Coles, Carolyn,Grishin, Anton,Kolesik, Peter,Tsanaktsidis, John,Kassiou, Michael
supporting information, p. 277 - 301 (2015/03/31)
Alpha7 nicotinic acetylcholine receptors (nAChRs) have implications in the regulation of cognitive processes such as memory and attention and have been identified as a promising therapeutic target for the treatment of the cognitive deficits associated with schizophrenia and Alzheimer's disease (AD). Structure affinity relationship studies of the previously described α7 agonist SEN12333 (8), have resulted in the identification of compound 45, a potent and selective agonist of the α7 nAChR with enhanced affinity and improved physicochemical properties over the parent compound (SEN12333, 8).
An electrochemical nickel-catalyzed arylation of 3-amino-6- chloropyridazines
Sengmany, Stephane,Vitu-Thiebaud, Arnaud,Le Gall, Erwan,Condon, Sylvie,Leonel, Eric,Thobie-Gautier, Christine,Pipelier, Muriel,Lebreton, Jacques,Dubreuil, Didier
, p. 370 - 379 (2013/03/13)
3-Amino-6-aryl- and 3-amino-6-heteroarylpyridazines have been obtained in generally good yield using a nickel-catalyzed electrochemical cross-coupling between 3-amino-6-chloropyridazines and aryl or heteroaryl halides at room temperature. Comparative experiments involving classical palladium-catalyzed reactions, such as Suzuki, Stille, or Negishi cross-couplings, reveal that the electrochemical method can constitute a reliable alternative tool for biaryl formation. A possible reaction mechanism is proposed on the basis of electrochemical analyses.