Carbazole-containing amides and ureas: Discovery of cryptochrome modulators as antihyperglycemic agents
A series of novel carbazole-containing amides and ureas were synthesized. A structure–activity relationship study of these compounds led to the identification of potent cryptochrome modulators. Based on the desired pharmacokinetic/pharmacodynamic parameters and the results of efficacy studies in db/db mice, compound 50 was selected for further profiling.
Humphries, Paul S.,Bersot, Ross,Kincaid, John,Mabery, Eric,McCluskie, Kerryn,Park, Timothy,Renner, Travis,Riegler, Erin,Steinfeld, Tod,Turtle, Eric D.,Wei, Zhi-Liang,Willis, Erik
p. 293 - 297
(2018/01/04)
Photochemical rearrangement of N -chlorolactams: A route to N -heterocycles through concerted ring contraction
We report a novel ring contraction allowing the direct conversion of N-chlorolactams to their corresponding ring-contraction N-heterocycles upon photolysis. Results show that the rearrangement occurs with a variety of N-chlorolactams and that the greater the substitution at the migrating carbon, the greater the yield of product. Importantly, stereochemistry at the migrating carbon is conserved in the product. Rearranged products were isolated as their methyl carbamates in yields varying from 17% to 58%, with the major side product being the recyclable parent lactam.
Winter, Dana K.,Drouin, Alexandre,Lessard, Jean,Spino, Claude
supporting information; experimental part
p. 2610 - 2618
(2010/06/17)
The synthesis and chemistry of 3-diazo-piperidin-2-one
The efficient synthesis of 3-diazo-piperidin-2-one, from L-ornithine, in two steps is reported. The chemistry of this new cyclic α-diazoamide was explored and allows the rapid access to a wide range of 3-substituted piperidin-2-one derivatives.
Hutchinson, Ian S,Matlin, Stephen A,Mete, Antonio
p. 3137 - 3143
(2007/10/03)
More Articles about upstream products of 25219-59-4