54934-30-4Relevant academic research and scientific papers
β-Enamino esters in heterocyclic synthesis: Synthesis of pyrazolone and pyridinone derivatives
Salaheldin, Abdellatif Mohamed,Al-Sheikh, Mariam Abdullah
experimental part, p. 4359 - 4368 (2010/10/01)
An efficient and convenient synthesis of pyrrolidinones and pyridinones utilizing enamino esters as starting material has been described. The structures of the compounds obtained were confirmed by spectral and elemental analyses.
Synthesis and biological evaluation of novel pyrazoles and indazoles as activators of the nitric oxide receptor, soluble guanylate cyclase
Selwood,Brummell,Budworth,Burtin,Campbell,Chana,Charles,Fernandez,Glen,Goggin,Hobbs,Kling,Liu,Madge,Meillerais,Powell,Reynolds,Spacey,Stables,Tatlock,Wheeler,Wishart,Woo
, p. 78 - 93 (2007/10/03)
Database searching and compound screening identified 1-benzyl-3-(3-dimethylaminopropyloxy)-indazole (benzydamine, 3) as a potent activator of the nitric oxide receptor, soluble guanylate cyclase. A comprehensive structure-activity relationship study surrounding 3 clearly showed that the indazole C-3 dimethylaminopropyloxy substituent was critical for enzyme activity. However replacement of the indazole ring of 3 by appropriately substituted pyrazoles maintained enzyme activity. Compounds were evaluated for inhibition of platelet aggregation and showed a general lipophilicity requirement. Aryl-substituted pyrazoles 32, 34, and 43 demonstrated potent activation of soluble guanylate cyclase and potent inhibition of platelet aggregation. Pharmacokinetic studies in rats showed that compound 32 exhibits modest oral bioavailability (12%) Furthermore 32 has an excellent selectivity profile notably showing no significant inhibition of phosphodiesterases or nitric oxide synthases.
