Design of non-peptide CCK2 and NK1 peptidomimetics using 1-(2-nitrophenyl)thiosemicarbazide as a novel common scaffold.
A beta-turn overlay hypothesis has been used to transform the core scaffold of a selective non-peptide bradykinin B2 receptor antagonist into ligands specifically recognized by the CCK2 or NK1 receptors.
Novartis Institute for Medical Sciences, London, UK. ed.dziadulewicz@pharma.novartis.com
E K
EK
Dziadulewicz
C S
CS
Walpole
C R
CR
Snell
R
R
Wrigglesworth
G A
GA
Hughes
D
D
Beattie
J N
JN
Wood
M M
MM
Beech
P R
PR
Coote
D000818:Animals; D001923:Brain Chemistry; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000737:chemistry; D066298:In Vitro Techniques; D008024:Ligands; D008958:Models, Molecular; D015394:Molecular Structure; D009574:Nitro Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism*; D010455:Peptides / Q000737:chemistry*; D011487:Protein Conformation; D011869:Radioligand Assay; D011949:Receptors, Cholecystokinin / Q000737:chemistry / Q000378:metabolism*; D018040:Receptors, Neurokinin-1 / Q000737:chemistry / Q000378:metabolism*; D012663:Semicarbazides / Q000737:chemistry*
D004791:Enzyme Inhibitors; D008024:Ligands; D009574:Nitro Compounds; D010455:Peptides; D011949:Receptors, Cholecystokinin; D018040:Receptors, Neurokinin-1; D012663:Semicarbazides; C005151:thiosemicarbazide