175203-64-2Relevant academic research and scientific papers
Highly chemoselective metal-free reduction of tertiary amides
Barbe, Guillaume,Charette, Andre B.
, p. 18 - 19 (2008/09/20)
This communication describes the chemoselective metal-free reduction of tertiary amides to the corresponding amines. Hantzsch ester is used as a mild reducing agent for the reduction of trifluoromethanesulfonic anhydride activated amides providing the tertiary amines with high functional group tolerance. Copyright
New 1-benzyl-4-hydroxypiperidine derivatives as non-imidazole histamine H3 receptor antagonists
Maslowska-Lipowicz, Iwona,Figlus, Marek,Zuiderveld, Obbe P.,Walczynski, Krzysztof
experimental part, p. 762 - 773 (2009/05/07)
A series of 1-benzyl-4-(3-aminopropyloxy)piperidine and 1-benzyl-4-(5-aminopentyloxy)piperidine derivatives has been prepared. The 1-benzyl-4-hydroxypiperidine derivatives obtained were evaluated for their affinities at recombinant human histamine H3 receptor, stably expressed in HEK 293T cells. All compounds investigated show moderate to pronounced in-vitro affinities. The most potent antagonists in this series 9b2 (hH3R, pKi = 7.09), 9b1 (hH3R, pKi = 6.78), 9b5 (hH3R, pKi = 6.99), and 9b6 (hH3R, pKi = 6.97) were also tested in vitro as H3 receptor antagonists - the electrically evoked contraction of the guinea-pig jejunum. The histaminergic H1 antagonism of selected compounds 9b1, 9b2, and 9b4-9b6 was established on the isolated guinea-pig ileum by conventional methods; the pA2 values were compared with the potency of pyrilamine. The compounds did not show any H1 antagonistic activity (pA 2 2 = 9.53).
Heterocyclic compounds as inhibitors of rotomase enzymes
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, (2008/06/13)
Compounds of the formula: wherein R1, Y, W, A and R2are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore moderate neuronal regeneration and outgrowth and can be used for treating neurological disorders arising from neurodegenerative diseases and nerve damage.
