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• W2019696218 abstract "Optimization of the R(2) and R(6) positions of (5-{4-[3-(R)-2-methylpyrrolin-1-yl-propoxy]phenyl}-2H-pyridazin-3-one) 2a with constrained phenoxypiperidines led to the identification of 5-[4-(cyclobutyl-piperidin-4-yloxy)-phenyl]-6-methyl-2H-pyridazin-3-one 8b as a potent, selective histamine H(3) receptor antagonist with favorable pharmacokinetic properties. Compound 8b had an excellent safety genotoxocity profile for a CNS-active compound in the Ames and micronucleus tests, also displayed potent H(3)R antagonist activity in the brain in the rat dipsogenia model and robust wake activity in the rat EEG/EMG model." @default.
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• W2019696218 date "2012-01-01" @default.
• W2019696218 modified "2023-09-26" @default.
• W2019696218 title "Synthesis and structure–activity relationship of 5-pyridazin-3-one phenoxypiperidines as potent, selective histamine H3 receptor inverse agonists" @default.
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• W2019696218 doi "https://doi.org/10.1016/j.bmcl.2011.11.118" @default.
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