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Synthesis and characterization of novel classes of PDE10A inhibitors - 1H-1,3-benzodiazoles and imidazo[1,2-a]pyrimidines.
Moszczynski-Petkowski, Rafal; Majer, Jakub; Borkowska, Malgorzata; Bojarski, Lukasz; Janowska, Sylwia; Matloka, Mikolaj; Stefaniak, Filip; Smuga, Damian; Bazydlo, Katarzyna; Dubiel, Krzysztof; Wieczorek, Maciej.
Afiliação
  • Moszczynski-Petkowski R; Celon Pharma S.A., Medicinal Chemistry Department, Mokra 41a, Kielpin, 05-092, Lomianki, Poland. Electronic address: rafal.moszczynski@celonpharma.com.
  • Majer J; Celon Pharma S.A., Medicinal Chemistry Department, Mokra 41a, Kielpin, 05-092, Lomianki, Poland.
  • Borkowska M; Celon Pharma S.A., Medicinal Chemistry Department, Mokra 41a, Kielpin, 05-092, Lomianki, Poland.
  • Bojarski L; Celon Pharma S.A., Innovative Drugs Research and Development Department, Mokra 41a, Kielpin, 05-092, Lomianki, Poland.
  • Janowska S; Celon Pharma S.A., Innovative Drugs Research and Development Department, Mokra 41a, Kielpin, 05-092, Lomianki, Poland.
  • Matloka M; Celon Pharma S.A., Innovative Drugs Research and Development Department, Mokra 41a, Kielpin, 05-092, Lomianki, Poland.
  • Stefaniak F; Celon Pharma S.A., Medicinal Chemistry Department, Mokra 41a, Kielpin, 05-092, Lomianki, Poland.
  • Smuga D; Celon Pharma S.A., Medicinal Chemistry Department, Mokra 41a, Kielpin, 05-092, Lomianki, Poland.
  • Bazydlo K; Celon Pharma S.A., Innovative Drugs Research and Development Department, Mokra 41a, Kielpin, 05-092, Lomianki, Poland.
  • Dubiel K; Celon Pharma S.A., Medicinal Chemistry Department, Mokra 41a, Kielpin, 05-092, Lomianki, Poland.
  • Wieczorek M; Celon Pharma S.A., Innovative Drugs Research and Development Department, Mokra 41a, Kielpin, 05-092, Lomianki, Poland.
Eur J Med Chem ; 155: 96-116, 2018 Jul 15.
Article em En | MEDLINE | ID: mdl-29870883
New compounds containing [1,2,4]triazolo [1,5-a]pyridine (I), pyrazolo [1,5-a]pyridine (II), 1H-1,3-benzodiazole (III) and imidazo [1,2-a]pyrimidine (IV) backbones were designed and synthesized for PDE10A interaction. Among these compounds, 1H-1,3-benzodiazoles and imidazo [1,2-a]pyrimidines showed the highest affinity for PDE10A enzyme as well as good metabolic stability. Both classes of compounds were identified as selective and potent PDE10A enzyme inhibitors.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirimidinas / Diester Fosfórico Hidrolases / Inibidores Enzimáticos Limite: Humans Idioma: En Revista: Eur J Med Chem Ano de publicação: 2018 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirimidinas / Diester Fosfórico Hidrolases / Inibidores Enzimáticos Limite: Humans Idioma: En Revista: Eur J Med Chem Ano de publicação: 2018 Tipo de documento: Article