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2' biaryl amides as novel and subtype selective M1 agonists. Part II: Further optimization and profiling.
Budzik, Brian; Garzya, Vincenzo; Shi, Dongchuan; Walker, Graham; Lauchart, Yann; Lucas, Adam J; Rivero, Ralph A; Langmead, Christopher J; Watson, Jeannette; Wu, Zining; Forbes, Ian T; Jin, Jian.
Afiliação
  • Budzik B; Discovery Research and Centers of Excellence for Drug Discovery, GlaxoSmithKline, Collegeville, PA 19426, USA. torqux@yahoo.com
Bioorg Med Chem Lett ; 20(12): 3545-9, 2010 Jun 15.
Article em En | MEDLINE | ID: mdl-20483599
ABSTRACT
Further optimization of the biaryl amide series via extensively exploring structure-activity relationships resulted in potent and subtype selective M(1) agonists exemplified by compounds 9a and 9j with good rat PK properties including CNS penetration. Synthesis, structure-activity relationships, subtype selectivity for M(1) over M(2-5), and DMPK properties of these novel compounds are described.
Assuntos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Limite: Animals Idioma: En Ano de publicação: 2010 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Limite: Animals Idioma: En Ano de publicação: 2010 Tipo de documento: Article