Selective inhibition of Helicobacter pylori methionine aminopeptidase by azaindole hydroxamic acid derivatives: Design, synthesis, in vitro biochemical and structural studies
Methionine aminopeptidases (MetAPs) are an important class of enzymes that work co-translationally for the removal of initiator methionine. Chemical inhibition or gene knockdown is lethal to the microbes suggesting that they can be used as antibiotic targ
Bala, Sandeepchowdary,Yellamanda, Kalisha vali,Kadari, Anilkumar,Ravinuthala, Venkata.S.U.,Kattula, Bhavita,Singh, Om V.,Gundla, Rambabu,Addlagatta, Anthony
Synthesis and evaluation of 5-fluoro-2-aryloxazolo[5,4- b ]pyridines as β-amyloid PET ligands and identification of MK-3328
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.
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.
experimental part
p. 498 - 502
(2011/09/14)
NOVEL SUBSTITUTED AZABENZOXAZOLES
The present invention relates to novel amyloid binding compounds and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the
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Page/Page column 29
(2010/01/12)
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