246034-30-0Relevant articles and documents
Synthesis and evaluation of 5-fluoro-2-aryloxazolo[5,4- b ]pyridines as β-amyloid PET ligands and identification of MK-3328
Harrison, Scott T.,Mulhearn, James,Wolkenberg, Scott E.,Miller, Patricia J.,O'Malley, Stacey S.,Zeng, Zhizhen,Williams Jr., David L.,Hostetler, Eric D.,Sanabria-Bohorquez, Sandra,Gammage, Linda,Fan, Hong,Sur, Cyrille,Culberson, J. Christopher,Hargreaves, Richard J.,Cook, Jacquelynn J.,Hartman, George D.,Barrow, James C.
supporting information; experimental part, p. 498 - 502 (2011/09/14)
5-Fluoro-2-aryloxazolo[5,4-b]pyridines were synthesized and investigated as potential 18F containing β-amyloid PET ligands. In competition binding assays using human AD brain homogenates, compounds 14b, 16b, and 17b were identified as having favorable potency versus human β-amyloid plaque and were radiolabeled for further evaluation in in vitro binding and in vivo PET imaging experiments. These studies led to the identification of 17b (MK-3328) as a candidate PET ligand for the clinical assessment of β-amyloid plaque load.
Synthesis of N-acetylglucosaminyl and diacetylchitobiosyl amides of heterocyclic carboxylic acids as potential chitinase inhibitors
Rottmann,Synstad,Eijsink,Peter
, p. 2293 - 2297 (2007/10/03)
2-(Dimethylammo)oxazoline-4-carboxylic acids 5 were prepared by condensation of binucleophilic amino acids 4 and O-ethyl-N,N-dimethyhsourea 3. New heterocyclic N-acetylglucosaminyl amides and chitobiosyl amides 8 were obtained by the coupling of tetraacetylglucosamine 6a or heptaacetylchitobiosylamine 6b with acid chlorides of heterocyclic carboxylic acids 2 or 5a and subsequent deacetylation. Based on their substitution patterns, compounds 8 were expected to have inhibitory activity towards chitinases. Enzyme assays showed that glycosyl amides 8 indeed were moderate inhibitors of chitinases, the diacetylchitobiosyl amides 8d-f generally having higher inhibitory activities than the N-acetylglucosaminyl amide derivatives 8a-c. Inhibitory activities depended on the chitinase tested.