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Substituted pyrazoles as novel sEH antagonist: investigation of key binding interactions within the catalytic domain.
Lo, Ho Yin; Man, Chuk C; Fleck, Roman W; Farrow, Neil A; Ingraham, Richard H; Kukulka, Alison; Proudfoot, John R; Betageri, Raj; Kirrane, Tom; Patel, Usha; Sharma, Rajiv; Hoermann, Mary Ann; Kabcenell, Alisa; Lombaert, Stéphane De.
Afiliação
  • Lo HY; Boehringer Ingelheim Pharmaceuticals Inc., Biomolecular Screening, 900 Ridgebury Rd., PO Box 368, Ridgefield, CT 06877, USA. ho-yin.lo@boehringer-ingelheim.com
Bioorg Med Chem Lett ; 20(22): 6379-83, 2010 Nov 15.
Article em En | MEDLINE | ID: mdl-20934334
ABSTRACT
A novel series of pyrazole sEH inhibitors is reported. Lead optimization efforts to replace the aniline core are also described. In particular, 2-pyridine, 3-pyridine and pyridazine analogs are potent sEH inhibitors with favorable CYP3A4 inhibitory and microsomal stability profiles.
Assuntos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirazóis / Inibidores Enzimáticos / Epóxido Hidrolases Limite: Humans Idioma: En Ano de publicação: 2010 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirazóis / Inibidores Enzimáticos / Epóxido Hidrolases Limite: Humans Idioma: En Ano de publicação: 2010 Tipo de documento: Article