188400-93-3Relevant articles and documents
Novel 2,4-disubstituted pyrimidines as potent, selective, and cell-permeable inhibitors of neuronal nitric oxide synthase
Mukherjee, Paramita,Li, Huiying,Sevrioukova, Irina,Chreifi, Georges,Martásek, Pavel,Roman, Linda J.,Poulos, Thomas L.,Silverman, Richard B.
, p. 1067 - 1088 (2015/03/04)
Selective inhibition of neuronal nitric oxide synthase (nNOS) is an important therapeutic approach to target neurodegenerative disorders. However, the majority of the nNOS inhibitors developed are arginine mimetics and, therefore, suffer from poor bioavai
Synthesis of pharmacologically relevant indoles with amine side chains via tandem hydroformylation/fischer indole synthesis
Schmidt, Axel M.,Eilbracht, Peter
, p. 5528 - 5535 (2007/10/03)
The sequence of hydroformylation and Fischer indole synthesis starting from amino olefins and aryl hydrazines is described. In a convergent manner, the two units bearing pharmacologically relevant substituents are assembled in the final indolization step. This modular and diversity-oriented approach to tryptamines and homotryptamines can be conducted in water and allows synthesis of branched and nonbranched tryptamines as well as tryptamine-based pharmaceuticals such as the 5-HT1D agonist L 775 606.
Substituted 1-indolylpropyl-4-phenethylpiperazadine derivatives
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, (2008/06/13)
A class of 1-?3-(1H-indol-3-yl)propyl!-4-(2-phenylethyl) piperazine derivatives, substituted at the 5-position of the indole nucleus by a five-membered heteroaromatic moiety, and on the phenyl ring of the phenethyl moiety by fluoro, chloro, trifluoromethyl, alkoxy or an oxazolidinone group and optionally by one or two further substituents, are selective agonists of 5-HT1 -like receptors, being potent agonists of the human 5-HT1D α receptor subtype while possessing at least a 10-fold selective affinity for the 5-HT1D α receptor subtype relative to the 5-HT1D α subtype; they are therefore usefull in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT1D receptor agonists.
