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- W1966761489 abstract "11β-HSD1 is increasingly seen as an attractive target for the treatment of type II diabetes and other elements of the metabolic syndrome. In this program of work we describe how a series of neutral 2-thioalkyl-pyridine 11β-HSD1 inhibitors were optimized in terms of their pharmacokinetic properties to give compounds with excellent bioavailability in both rat and dog through a core change to pyrimidine. A potential reactive metabolite issue with 4-thioalkyl-pyrimidines was circumvented by a switch from sulfur to carbon substitution." @default.
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- W1966761489 date "2012-11-01" @default.
- W1966761489 modified "2023-10-10" @default.
- W1966761489 title "Optimisation of pharmacokinetic properties in a neutral series of 11β-HSD1 inhibitors" @default.
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- W1966761489 doi "https://doi.org/10.1016/j.bmcl.2012.08.070" @default.
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