Goldberg, Frederick W. published the artcileOptimization of Brain Penetrant 11¦Â-Hydroxysteroid Dehydrogenase Type I Inhibitors and in Vivo Testing in Diet-Induced Obese Mice, Formula: C3H8N2S, the publication is Journal of Medicinal Chemistry (2014), 57(3), 970-986, database is CAplus and MEDLINE.
11¦Â-Hydroxysteroid dehydrogenase type 1 (11¦Â-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 I, which had modest CNS penetration. More significant progress was achieved by changing the core to give II, which combines good potency and CNS penetration. Compound II was dosed to diet-induced obese (DIO) mice and gave excellent target engagement in the liver and high free exposures of drug, both peripherally and in the CNS. However, no body weight reduction or effects on glucose or insulin were observed in this model. Similar data were obtained with a structurally diverse thiazole compound III. This work casts doubt on the hypothesis that localized tissue modulation of 11¦Â-HSD1 activity alleviates metabolic syndrome.
Journal of Medicinal Chemistry published new progress about 6972-05-0. 6972-05-0 belongs to catalysis-chemistry, auxiliary class Thiourea,Amine,Aliphatic hydrocarbon chain,Amide, name is 1,1-Dimethylthiourea, and the molecular formula is C3H8N2S, Formula: C3H8N2S.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia