603941-89-5Relevant 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.
