Optimization of brain penetrant 11β-hydroxysteroid dehydrogenase type I inhibitors and in vivo testing in diet-induced obese mice.

@article{Goldberg2014OptimizationOB,
  title={Optimization of brain penetrant 11β-hydroxysteroid dehydrogenase type I inhibitors and in vivo testing in diet-induced obese mice.},
  author={Frederick W Goldberg and Alexander G Dossetter and James S Scott and Graeme R Robb and Scott Boyd and Sam D Groombridge and Paul D. Kemmitt and Tove Sj{\"o}gren and Pablo Morentin Gutierrez and Joanne Deschoolmeester and John G Swales and Andrew V. Turnbull and Martin J. Wild},
  journal={Journal of medicinal chemistry},
  year={2014},
  volume={57 3},
  pages={970-86}
}
11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) has been widely considered by the pharmaceutical industry as a target to treat metabolic syndrome in type II diabetics. We hypothesized that central nervous system (CNS) penetration might be required to see efficacy. Starting from a previously reported pyrimidine compound, we removed hydrogen-bond donors to yield 3, which had modest CNS penetration. More significant progress was achieved by changing the core to give 40, which combines good… CONTINUE READING

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