62902-66-3Relevant academic research and scientific papers
N-PHENYL-2-(3-PHENYL-6-OXO-1,6-DIHYDROPYRIDAZIN-1-YL)ACETAMIDE DERIVATIVES FOR TREATING CYSTIC FIBROSIS
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Paragraph 0123, (2018/05/24)
The present disclosure is directed to compounds that modulate, e.g., address underlying defects in cellular processing of CFTR (cystic fibrosis transmembrane conductance regulator) activity.
Synthesis and Bioevaluation of 3,6-Diaryl-[1,2,4]triazolo[4,3-b] Pyridazines as Antitubulin Agents
Xu, Qile,Wang, Yueting,Xu, Jingwen,Sun, Maolin,Tian, Haiqiu,Zuo, Daiying,Guan, Qi,Bao, Kai,Wu, Yingliang,Zhang, Weige
supporting information, p. 1202 - 1206 (2016/12/18)
A series of 3,6-diaryl-[1,2,4]triazolo[4,3-b]pyridazines were designed as a class of vinylogous CA-4 analogues. The easily isomerized (Z,E)-butadiene linker of vinylogous CA-4 was replaced by a rigid [1,2,4]triazolo[4,3-b]pyridazine scaffold. Twenty-one target compounds were synthesized and exhibited moderate to potent antiproliferative activity. The compound 4q with a 3-amino-4-methoxyphenyl moiety as the B-ring, comparable to CA-4 (IC50 = 0.009-0.012 μM), displayed the highly active antiproliferative activity against SGC-7901, A549, and HT-1080 cell lines with IC50 values of 0.014, 0.008, and 0.012 μM, respectively. Tubulin polymerization experiments indicated that 4q effectively inhibited tubulin polymerization, and immunostaining assay revealed that 4q significantly disrupted tubulin microtubule dynamics. Moreover, cell cycle studies revealed that compound 4q dramatically arrested cell cycle progression at G2/M phase in A549 cells. Molecular modeling studies showed that 4q could bind to the colchicine binding site on microtubules.
Discovery of substituted 6-pheny-3H-pyridazin-3-one derivatives as novel c-Met kinase inhibitors
Kang, Seung-Tae,Kim, Eun-Young,Archary, Raghavendra,Jung, Heejung,Park, Chi Hoon,Yun, Chang-Soo,Hwang, Jong Yeon,Choi, Sang Un,Chae, Chonghak,Lee, Chong Ock,Kim, Hyoung Rae,Ha, Jae Du,Ryu, Dohyun,Cho, Sung Yun
supporting information, p. 5093 - 5097 (2014/12/11)
We report a series of phenyl substituted pyridazin-3-ones substituted with morpholino-pyrimidines. The SAR of the phenyl was explored and their c-Met kinase and cell-based inhibitory activity toward c-Met driven cell lines were evaluated. Described herein
Copper-catalyzed aerobic dehydrogenation of C-C to C=C bonds in the synthesis of pyridazinones
Liang, Lei,Yang, Guanyu,Xu, Fengrong,Niu, Yan,Sun, Qi,Xu, Ping
supporting information, p. 6130 - 6136 (2013/09/24)
A simple and efficient procedure for the synthesis of pyridazin-3(2H)-ones through copper-catalyzed dehydrogenation of a single C-C bond of 4,5-dihydropyridazin-3(2H)-ones to a C=C bond with oxygen as the terminal oxidant is described. Functional groups including hydroxy, carboxylic, bromo, chloro, cyano, nitro and alkoxy were all tolerated under the reaction conditions. Moreover, this methodology was applied to the preparation of a series of structurally similar N-substituted 6-phenylpyridazinone compounds containing fluorine. The dehydrogenation reactions exhibit good yields and selectivity. Copper-catalyzed dehydrogenation of a C-C bond of 4,5-dihydropyridazinones to a C=C bond with oxygen as the terminal oxidant is described. Various functional groups were tolerated under the reaction conditions. The method was also applied to the preparation of a series of N-substituted 6-phenylpyridazinones containing fluoride. The dehydrogenation reactions exhibit good yields and selectivity.
PYRIDAZIN-3 (2H) -ONE DERIVATIVES AND THEIR USE AS PDE4 INHIBITORS
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Page/Page column 70, (2008/06/13)
New pyridazin-e-(2H)-one derivatives having the chemical structure of general formula (I) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of phosphodiesterase 4.
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.
Agricultural fungicidal compositions containing 6-(substituted phenyl)-pyridazinones and said pyridazinones
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, (2008/06/13)
Agricultural fungicidal compositions containing as an active ingredient one or more of 6-(substitutedphenyl)-3(2H)-pyridazinone compounds, salts thereof and 6-(substituted-phenyl)-4,5-dihydro-3(2H)-pyridazinone compounds, as well as new pyridazinone compo
