114872-56-9Relevant 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.
Synthesis of chirally pure 2,5-disubstituted diketopiperazines derived from trisubstituted phenylalanines
Danthi, Satyavijayan Narasimhan,Hill, Ronald A.
, p. 835 - 844 (2007/10/03)
Some new chirally pure 2,5-substituted diketopiperazines were synthesized starting from 2-methoxybenzyl alcohol. This multistep synthesis proceeds through the enzymatic synthesis of chirally pure amino acids, protection and dipeptide coupling, cyclization of dipeptide ester formates, and nitration of the resulting diketopiperazines.
