87769-63-9Relevant academic research and scientific papers
5-Amino-6-phenyl-1,6-dihydropyridazin-3(2H)-one
Novoa De Armas, Hector,Blaton, Norbert M.,Peeters, Oswald M.,De Ranter, Camiel J.,Pita, Beatriz,Sotelo, Eddy,Ravina, Enrique,Suarez, Margarita
, p. 345 - 346 (2000)
In the title compound, C10H9N3O, the pyridazinone moiety is essentially planar and forms a dihedral angle of 49.5 (1)° with the phenyl substituent. The molecular packing is stabilized by van der Waals interactions and hydr
Ureido-Pyridazinone Derivatives: Insights into the Structural and Conformational Properties for STAT3 Inhibition
Meneghetti, Fiorella,Villa, Stefania,Masciocchi, Daniela,Barlocco, Daniela,Toma, Lucio,Han, Dong-Cho,Kwon, Byoung-Mog,Ogo, Naohisa,Asai, Akira,Legnani, Laura,Gelain, Arianna
supporting information, p. 4907 - 4912 (2015/08/03)
Three new ureido-pyridazinone derivatives, which are structurally related to the known STAT3 inhibitor AVS-0288, were designed by taking into account the structure-activity relationships determined for several ureido-oxadiazole derivatives previously studied by our group. Their synthesis was first attempted through suitable 5-aminopyridazinone intermediates (6a and 6b), which molecular structures were confirmed by means of X-ray diffraction data on 6a. Amine functionalization was unsuccessful, therefore, an alternative method was devised. Dual-luciferase and AlphaScreen-based assays were used to test their activity. The obtained data were rationalized on the basis of a modeling study, which focused our attention on the geometrical preferences of the ureido moiety. Computational results seem to indicate that both the 1,2,5-oxadiazole ring and the extended ZZ arrangement are essential and probably act in a synergistic way to confer significant activity against STAT3.
Pyridazines. Part XXIX: Synthesis and platelet aggregation inhibition activity of 5-substituted-6-phenyl-3(2H)-pyridazinones. Novel aspects of their biological actions
Sotelo, Eddy,Fraiz, Nuria,Yáez, Matilde,Terrades, Vicente,Laguna, Reyes,Cano, Ernesto,Ravia, Enrique
, p. 2873 - 2882 (2007/10/03)
A series of 6-phenyl-3(2H)-pyridazinones with a diverse range of substituents in the 5-position have been prepared and evaluated in the search for new antiplatelet agents. A significant dependence of the substituent on the inhibitory effect has been observed. The pharmacological study of these compounds confirms that modification of the chemical group at position 5 of the 6-phenyl-3(2H)-pyridazinone system influences both variations in the antiplatelet activity and the mechanism of action.
Pyridazine derivatives. XIX: Functionalization studies at the 5 position in the 6-phenyl-3(2H)-pyridazinone system
Sotelo, Eddy,Ravina, Enrique,Estevez, Isabel
, p. 985 - 990 (2007/10/03)
A series of 6-phenyl-3(2H)-pyridazinones bearing different substitution at the 5 position of the pyridazinone ring were prepared in the search for new platelet aggregation inhibitors. The structure of the final compounds was determined on the basis of spectroscopics methods.
Pyridazines. XV. Synthesis of 6-aryl-5-amino-3(2H)-pyridazinones as potential platelet aggregation inhibitors
Estevez, Isabel,Ravina, Enrique,Sotelo, Eddy
, p. 1421 - 1428 (2007/10/03)
Several 3(2H)-pyridazinones with amino groups at the 5-position of the pyridazine nucleus have been prepared. The 6-aryl-5-halo-3(2H)-pyridazinones obtained from mucochloric and mucobromic acid lead to the corresponding 5- alkylamino-3(2H)-pyridazinones,
Synthesis of Aminopyridazines from Azidopyridazines and Tetrazolopyridazines
Kappe, Th.,Pfaffenschlager, A.,Stadlbauer, W.
, p. 666 - 671 (2007/10/02)
Azidopyridazines 3, 4, 24 and tetrazolopyridazines 10, 13, 28 can be converted to the corresponding aminopyridazines, by reaction with triphenylphosphine via phosphazenes and subsequent hydrolysis (Staudinger reaction).
