126337-04-0Relevant academic research and scientific papers
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.
PYRROLIDINYL UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS
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Paragraph 00628, (2014/06/11)
Compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R1, R2, Ra, Rb, Rc, Rd, X, Ring B, and Ring C are as defined herein, and wherein Ring B moiety and the NH-C(=X)-NH moiety are in the trans configuration, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.
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.
Ring Closure of 4-Azido-3-phenyl-pyridazines to Pyridazinoindoles
Stadlbauer, W.,Pfaffenschlager, A.,Kappe, Th.
, p. 781 - 783 (2007/10/02)
The cyclization of 4-azido-3-phenylpyridazines and 7-azido-6-phenyltetrazolopyridazine by heating with strong acids like methanesulfonic acid affords 5H-pyridazinoindoles or 10H-tetrazolopyridazinoindoles, respectively, whe
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).
