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- W2000206780 abstract "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." @default.
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- W2000206780 date "2010-09-01" @default.
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- W2000206780 title "Discovery of substituted benzyl tetrazoles as histamine H3 receptor antagonists" @default.
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- W2000206780 doi "https://doi.org/10.1016/j.bmcl.2010.07.009" @default.
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