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Discovery of IDO1 inhibitors containing a decahydroquinoline, decahydro-1,6-naphthyridine, or octahydro-1H-pyrrolo[3,2-c]pyridine scaffold.
Yu, Wensheng; Deng, Yongqi; Sloman, David; Li, Derun; Liu, Kun; Fradera, Xavier; Lesburg, Charles A; Martinot, Theo; Doty, Amy; Ferguson, Heidi; Richard Miller, J; Knemeyer, Ian; Otte, Karin; Vincent, Stella; Sciammetta, Nunzio; Jonathan Bennett, David; Han, Yongxin.
Afiliação
  • Yu W; Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA. Electronic address: wenshengyu@msn.com.
  • Deng Y; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Sloman D; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Li D; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Liu K; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Fradera X; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Lesburg CA; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Martinot T; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Doty A; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Ferguson H; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Richard Miller J; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Knemeyer I; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Otte K; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Vincent S; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Sciammetta N; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Jonathan Bennett D; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Han Y; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Bioorg Med Chem Lett ; 49: 128314, 2021 10 01.
Article em En | MEDLINE | ID: mdl-34391891
ABSTRACT
A series of IDO1 inhibitors containing a decahydroquinoline, decahydro-1,6-naphthyridine, or octahydro-1H-pyrrolo[3,2-c]pyridine scaffold were identified with good cellular and human whole blood activity against IDO1. These inhibitors contain multiple chiral centers and all diastereomers were separated. The absolute stereochemistry of each isomers were not determined. Compounds 15 and 27 stood out as leads due to their good cellular as well as human whole blood IDO1 inhibition activity, low unbound clearance, and reasonable mean residence time in rat cassette PK studies.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirróis / Quinolinas / Inibidores Enzimáticos / Indolamina-Pirrol 2,3,-Dioxigenase / Naftiridinas Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2021 Tipo de documento: Article
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirróis / Quinolinas / Inibidores Enzimáticos / Indolamina-Pirrol 2,3,-Dioxigenase / Naftiridinas Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2021 Tipo de documento: Article