Discovery and optimization of adamantyl carbamate inhibitors of 11灏?HSD1 was written by Tice, Colin M.;Zhao, Wei;Krosky, Paula M.;Kruk, Barbara A.;Berbaum, Jennifer;Johnson, Judith A.;Bukhtiyarov, Yuri;Panemangalore, Reshma;Scott, Boyd B.;Zhao, Yi;Bruno, Joseph G.;Howard, Lamont;Togias, Jennifer;Ye, Yuan-Jie;Singh, Suresh B.;McKeever, Brian M.;Lindblom, Peter R.;Guo, Joan;Guo, Rong;Nar, Herbert;Schuler-Metz, Annette;Gregg, Richard E.;Leftheris, Katerina;Harrison, Richard K.;McGeehan, Gerard M.;Zhuang, Linghang;Claremon, David A.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2010.Category: pyridine-derivatives This article mentions the following:
Synthesis of 2-adamantyl carbamate derivatives of piperidines and pyrrolidines led to the discovery of 2-adamantanyl (3R)-3-tert.-butoxycarbonylaminopyrrolidine-1-carboxylate with an IC50 of 15.2 nM against human 11灏?HSD1 in adipocytes. Optimization for increased adipocyte potency, metabolic stability and selectivity afforded 1-carbamoyladmanatan-4-yl (3R)-(3-cyano- and 5-cyanopyrdinylamino)pyrrolidine-1-carboxylate, both of which were >25% orally bioavailable in rat. In the experiment, the researchers used many compounds, for example, 2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0Category: pyridine-derivatives).
2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0) belongs to pyridine derivatives. Pyridine has a conjugated system of six 锜?electrons that are delocalized over the ring. The molecule is planar and, thus, follows the H鐪塩kel criteria for aromatic systems. Pyridine groups exist in countless molecules, and their applications include catalysis, drug design, molecular recognition, and natural product synthesis.Category: pyridine-derivatives