78784-65-3Relevant academic research and scientific papers
EAAT2 ACTIVATORS AND METHODS OF USING THEREOF
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Page/Page column 83-84, (2019/12/28)
Disclosed are compounds that activate excitatory amino acid transporter 2 (EAAT2), as well as methods of using these compounds to treat or preventing diseases, disorders, and conditions associated with glutamate excitotoxicity.
Discovery of substituted pyrazol-4-yl pyridazinone derivatives as novel c-Met kinase inhibitors
Kim, Eun-Young,Kang, Seung-Tae,Jung, Heejung,Park, Chi Hoon,Yun, Chang-Soo,Hwang, Jong Yeon,Byun, Byung Jin,Lee, Chong Ock,Kim, Hyoung Rae,Ha, Jae Du,Ryu, Do Hyun,Cho, Sung Yun
, p. 453 - 464 (2016/04/26)
A series of pyridazin-3-one substituted with morpholino-pyrimidine derivatives was synthesized and evaluated as tyrosine kinase inhibitors against c-Met enzyme, and anti-proliferative activities of Hs746T human gastric cancer cell line. Most of compounds exhibited good biological activity, while compound 10, 12a, 14a displayed excellent c-Met enzyme inhibitory activities and Hs746T cell-based activities.
Structure-activity relationship study of pyridazine derivatives as glutamate transporter EAAT2 activators
Xing, Xuechao,Chang, Ling-Chu,Kong, Qiongman,Colton, Craig K.,Lai, Liching,Glicksman, Marcie A.,Lin, Chien-Liang Glenn,Cuny, Gregory D.
scheme or table, p. 5774 - 5777 (2011/10/18)
Excitatory amino acid transporter 2 (EAAT2) is the major glutamate transporter and functions to remove glutamate from synapses. A thiopyridazine derivative has been found to increase EAAT2 protein levels in astrocytes. A structure-activity relationship study revealed that several components of the molecule were required for activity, such as the thioether and pyridazine. Modification of the benzylthioether resulted in several derivatives (7-13, 7-15 and 7-17) that enhanced EAAT2 levels by >6-fold at concentrations 50 of 0.5 μM.
COUPLING OF ORGANOTIN REAGENTS WITH ARYL, ACYL AND HETEROARYL HALIDES: SYNTHESIS OF PYRIDAZINE AND QUINOXALONE DERIVATIVES
Powell, Paul,Sosabowski, Michael H.
, p. 2422 - 2434 (2007/10/03)
Couplin of organotin reagents Bu3SnAr (Ar = 2- or 3-thienyl, 2- or 3-pyridyl) with ClCOCH2CH2CO2Et in the presence of PdCl(CH2Ph)(PPh3)2 yields β-ketoesters ArCOCH2CH2CO2Et which were converted with hydrazine hydrate into 6-substituted 4,5-dihydropyridazin-3(2H)-ones, and thence to 3-halogeno-6-substituted pyridazines.The latter also couple under similar conditions with Bu3SnAr to yield 3-heteroarylpyridazines.With catalysts, coupling of ClCOCO2Et and Bu3SnAr proceeds with loss of carbon monoxide giving ArCO2Et, but without catalyst ArCOCO2Et is formed from which the3-heteroarylquinoxalin-3-one is prepared.The reactions of Bu3SnAr with 4-XC6H4Br (X = H,-OMe, -CN, -NO2) are also described.
Novel antiasthmatic agents with dual activities of thromboxane A2 synthetase inhibition and bronchodilation. IV. 2-[2-(1-imidazolyl)ethyl]-4-(3-pyridyl)-1(2H)-phthalazinones
Yamaguchi,Koga,Kamei,Akima,Maruyama,Kuroki,Hamana,Ohi
, p. 1850 - 1853 (2007/10/02)
Synthesis and pharmacological evaluation of several compounds related to 2-[2-(1-imidazolyl)ethyl]-4-(3-pyridyl)-1(2H)-phthalazinones are described. The phenyl moiety of the phthalazinone skeleton was found to play an important role in both thromboxane A
One-pot preparation of 6-substituted 3(2H)-pyridazinones from ketones
Coates,McKillop
, p. 334 - 342 (2007/10/02)
A one-pot process for the preparation of 6-phenyl-3(2H)-pyridazinone from acetophenone and glyoxylic acid has been investigated and shown to have wide utility in the preparation of 6- and 5,6-substituted 3(2H)-pyridazinones. Limitations to the process encountered with 2'-hydroxyacetophenone and with basic hetero-aromatic ketones have been overcome, and the processes described offer the rapid and efficient synthesis of many 6-substituted pyridazinones from readily available ketones.
6- And 8-heteroaryl-1,2,4-triazolo[4,3-b]pyridazines
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, (2008/06/13)
This disclosure describes novel 6- and 8-heteroaryl and substituted 6- and 8-heteroaryl-1,2,4-triazolo[4,3-b]-pyridazines and their use as agents for treating anxiety.
