Beta 3 agonists. Part 1: evolution from inception to BMS-194449.
Bioorg Med Chem Lett
; 11(23): 3035-9, 2001 Dec 03.
Article
em En
| MEDLINE
| ID: mdl-11714605
ABSTRACT
Screening of the BMS collection identified 4-hydroxy-3-methylsulfonanilidoethanolamines as full beta 3 agonists. Substitution of the ethanolamine nitrogen with a benzyl group bearing a para hydrogen bond acceptor promoted beta(3) selectivity. SAR elucidation established that highly selective beta(3) agonists were generated upon substitution of C(alpha) with either benzyl to form (R)-1,2-diarylethylamines or with aryl to generate 1,1-diarylmethylamines. This latter subset yielded a clinical candidate, BMS-194449 (35).(1)
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Agonistas Adrenérgicos beta
/
Etanolamina
/
Agonistas de Receptores Adrenérgicos beta 3
/
Anilidas
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2001
Tipo de documento:
Article
País de afiliação:
Estados Unidos