Synthesis, molecular modelling and biological activity of some pyridazinone derivatives as selective human monoamine oxidase-B inhibitors
Background: Since brain neurotransmitter levels are associated with the pathology of various neurodegenerative diseases like Parkinson and Alzheimer, monoamineoxidase (MAO) plays a critical role in balancing these neurotransmitters in the brain. MAO isofo
?zdemir, Zeynep,Alag?z, Mehmet Abdullah,Uslu, Harun,Karakurt, Arzu,Erikci, Acelya,Ucar, Gulberk,Uysal, Mehtap
p. 692 - 704
(2020/03/11)
The novel synthesized pyridazinone derivates had the antiproliferative and apoptotic effects in SHSY5Y and HEP3B cancer cell line
Background: Brain cancer (neuroblastoma) and liver cancer (hepatocellular carcinoma) are common cancer types among others worldwide which do not have a radical treatment and cure. Objective: In the current study, five novel pyridazinone derivates bearing
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
Sengmany, Stéphane,Lebre, Julie,Le Gall, Ewan,Léonel, Eric
p. 4859 - 4867
(2015/08/03)
An electrochemical nickel-catalyzed arylation of 3-amino-6- chloropyridazines
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.
Synthesis and antimicrobial, acetylcholinesterase and butyrylcholinesterase inhibitory activities of novel ester and hydrazide derivatives of 3(2H)-pyridazinone
In the current study, some novel ethyl 6-[(substituted-phenylpiperazine]- 3(2H)-pyridazinone-2-yl propionate III and 6-[(substituted-phenylpiperazine]- 3(2H)-pyridazinone-2-yl propionohydrazide IV derivatives were synthesized as acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitors. The structures of these new pyridazinone derivatives were confirmed by their IR, 1H-NMR spectra and elementary analysis. 6-Substituted-3(2H)- pyridazinone-2-yl propionate IIIa-e derivatives showed significant inhibitory activity against AChE and BChE. 6-[4-(3-Trifluoromethylphenyl)-piperazine]-3(2H) -pyridazinone-2-yl propionate IIIe has been found to be the most active compound in terms of inhibition of either AChE or BChE. Compound IIIe exhibited inhibitory activity close to that of galantamine (CAS 357-70-0) and did not show any selectivity between the two enzymes. Also the antimicrobial activities of III and IV derivatives have been evaluated. All III and IV derivatives exhibited poor antibacterial activities but moderate antifungal activities. ECV ? Editio Cantor Verlag.
Oezcelik, Azime Berna,Goekce, Mehtap,Orhan, Ilkay,Kaynak, Fatma,Sahin, Mustafa Fethi
scheme or table
p. 452 - 458
(2011/04/25)
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