Design of non-peptide CCK2 and NK1 peptidomimetics using 1-(2-nitrophenyl)thiosemicarbazide as a novel common scaffold

E K Dziadulewicz; C S Walpole; C R Snell; R Wrigglesworth; G A Hughes; D Beattie; J N Wood; M M Beech; P R Coote

doi:10.1016/s0960-894x(01)00044-0

Design of non-peptide CCK2 and NK1 peptidomimetics using 1-(2-nitrophenyl)thiosemicarbazide as a novel common scaffold

Bioorg Med Chem Lett. 2001 Mar 12;11(5):705-9. doi: 10.1016/s0960-894x(01)00044-0.

Authors

E K Dziadulewicz¹, C S Walpole, C R Snell, R Wrigglesworth, G A Hughes, D Beattie, J N Wood, M M Beech, P R Coote

Affiliation

¹ Novartis Institute for Medical Sciences, London, UK. ed.dziadulewicz@pharma.novartis.com

PMID: 11266174
DOI: 10.1016/s0960-894x(01)00044-0

Abstract

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.

MeSH terms

Animals
Brain Chemistry
Drug Design
Enzyme Inhibitors / chemistry
In Vitro Techniques
Ligands
Models, Molecular
Molecular Structure
Nitro Compounds / chemical synthesis
Nitro Compounds / chemistry*
Nitro Compounds / metabolism*
Peptides / chemistry*
Protein Conformation
Radioligand Assay
Receptors, Cholecystokinin / chemistry
Receptors, Cholecystokinin / metabolism*
Receptors, Neurokinin-1 / chemistry
Receptors, Neurokinin-1 / metabolism*
Semicarbazides / chemistry*

Substances

Enzyme Inhibitors
Ligands
Nitro Compounds
Peptides
Receptors, Cholecystokinin
Receptors, Neurokinin-1
Semicarbazides
thiosemicarbazide