177842-12-5Relevant articles and documents
Anthranilic acid based CCK1 receptor antagonists: Preliminary investigation on their second "touch point"
Varnavas, Antonio,Lassiani, Lucia,Valenta, Valentina,Mennuni, Laura,Makovec, Francesco,Hadjipavlou-Litina, Dimitra
, p. 563 - 581 (2007/10/03)
In this phase of structure-affinity relationship study of VL-0395, a new anthranilic acid based CCK1 selective antagonist, we propose a series of unnatural aminoacidic derivatives. The result of this work is the identification of a new CCK ligand, which possesses an affinity (IC50 = 35 nm) one order of magnitude greater than the lead and, as a general rule, it points out how the hypothesized receptorial pocket which accommodates the Phe residue allows much more structural modification than that interacting with the N-terminal group. Hence, the modification of the C-terminal pharmacophoric group of our lead VL-0395 can not only enhance the affinity of anthranilic acid derivatives but can modulate the selectivity for one CCK receptor subtype or afford mixed antagonists.
A convenient preparation of 4-t-butyl-L-phenylalanine
Jiang, Jianjun,Miller, Robert B.,Tolle, John C.
, p. 3015 - 3019 (2007/10/03)
A convenient preparation of 4-t-butyl-L-phenylalanine and N-Fmoc-4-t- butyl-L-phenylalanine are described.
