263410-21-5Relevant articles and documents
Synthesis and evaluation of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 3: Heterocyclic P3
Tully, David C.,Liu, Hong,Alper, Phil B.,Chatterjee, Arnab K.,Epple, Robert,Roberts, Michael J.,Williams, Jennifer A.,Nguyen, Khanhlinh T.,Woodmansee, David H.,Tumanut, Christine,Li, Jun,Spraggon, Glen,Chang, Jonathan,Tuntland, Tove,Harris, Jennifer L.,Karanewsky, Donald S.
, p. 1975 - 1980 (2006)
A series of Nα-2-benzoxazolyl-α-amino acid-(arylaminoethyl)amides were identified as potent, selective, and noncovalent inhibitors of cathepsin S. Structure-activity relationships including strategies for modulating the selectivities among cathepsins S, K, and L, and in vivo pharmacokinetics are discussed. A X-ray structure of compound 3 bound to the active site of cathepsin S is also reported.
Synthesis of chiral iminoalkyl functionalised N-heterocyclic carbenes and their use in asymmetric catalysis
Merzouk, Mahboub,Moore, Theo,Williams, Neil A.
, p. 8914 - 8917 (2008/03/14)
A library of new chiral iminoalkyl imidazolium salts has been synthesised from amino acids using a modular design approach. Deprotonation with silver oxide yields silver carbene transfer reagents, which can be used as ligand sources in asymmetric catalysis. Preliminary testing has shown that the ligands induce enantioselectivity in the palladium-catalysed allylic alkylation of 1,3-diphenylprop-3-enyl acetate with dimethyl malonate.
