1177252-58-2Relevant academic research and scientific papers
Discovery of substituted benzyl tetrazoles as histamine H3 receptor antagonists
Davenport, Adam J.,Stimson, Christopher C.,Corsi, Massimo,Vaidya, Darshan,Glenn, Edward,Jones, Timothy D.,Bailey, Sarah,Gemkow, Mark J.,Fritz, Ulrike,Hallett, David J.
scheme or table, p. 5165 - 5169 (2010/10/20)
A series of potent and subtype selective H3 receptor antagonists containing a novel tetrazole core and diamine motif is reported. A one-pot multi-component Ugi reaction was utilised to rapidly develop the structure-activity relationships (SAR) of these compounds. Optimisation for liver microsome stability (t1/2 >60 min), minimal CYP inhibition (IC50 >50 μM) and high cell permeability (Caco-2 Papp >20 × 10-6 cm/s) identified several compounds with drug-like properties.
DIAZEPANES AS HISTAMINE H3 RECEPTOR ANTAGONISTS
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Page/Page column 98; 107, (2009/09/05)
The invention relates to compounds of formula (I) wherein R1 to R8 and X1, X2 have the meaning as cited in the description and the claims. Said compounds are useful as Histamine H3 receptor antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
