200868-41-3Relevant academic research and scientific papers
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).
Pyridyl alkane acid amides as cytostatics and immunosupressives
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, (2008/06/13)
The invention relates to new pyridyl alkane acid amides according to general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical use, especially in the treatment of tumors or for immunosuppr
Pyridyl alkane acid amides as cytostatics and immunosuppressives
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, (2008/06/13)
The invention relates to new pyridyl alkane acid amides according to general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical use, especially in the treatment of tumors or for immunosuppr
Use of pyridyl alkane, pyridyl alkene and/or pyridyl alkine acid amides in the treatment of tumors or for immunosuppression
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, (2008/06/13)
The invention relates to the use of pharmacologically valuable pyridyl alkane, pyridyl alkene and/or pyridyl alkine acid amides according to general formula (I) in the treatment of tumors or for immunosuppression.
