856570-89-3Relevant academic research and scientific papers
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.
THE ANALOGS OF 8-D-HOMOARGININ-VASOPRESSIN WITH o-SUBSTITUTED PHENYLALANINE IN POSITION 2: SYNTHESIS AND SOME BIOLOGICAL PROPERTIES
Zertova, Miroslava,Prochazka, Zdenko,Slaninova, Jirina,Barth, Tomislav,Majer, Pavel,Lebl, Michal
, p. 1103 - 1110 (2007/10/02)
Solid phase methodology on p-methylbenzhydrylamine resin was used for the synthesis of four analogs of vasopressin with the non coded amino acids, D-homoarginine (in position 8) and o-substitued L- or D-phenylalanine (in position 2). 2/s
