II. Discovery of a novel series of CXCR3 antagonists with a beta amino acid core.
Bioorg Med Chem Lett
; 26(22): 5429-5437, 2016 11 15.
Article
em En
| MEDLINE
| ID: mdl-27789141
ABSTRACT
A new series of beta amino acids, which act as CXCR3 antagonists, has been identified. The formerly optimized N,N-disubstituted benzylamine derivatives with carboxylic acid function on the N-atom was used as starting point and compounds with carboxyl function not attached to the N-atom were investigated. Affinity, metabolic stability in human and mouse liver microsomes and Caco-2 permeability were optimized. Compounds with double-digit nanomolar CXCR3 affinity, favourable microsomal stability and Caco-2 permeability have been identified.
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Base de dados:
MEDLINE
Assunto principal:
Benzilaminas
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Receptores CXCR3
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Aminoácidos
Limite:
Animals
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Humans
Idioma:
En
Ano de publicação:
2016
Tipo de documento:
Article