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Discovery of novel pyrimidine and malonamide derivatives as TGR5 agonists.
Park, Eun Ju; Ahn, Young Gil; Jung, Seung Hyun; Bang, Hyo Jeong; Kim, Mira; Hong, Dong Jin; Kim, Jisook; Suh, Kwee Hyun; Kim, Young Jin; Kim, Doran; Kim, Eun-Yeong; Lee, Kiho; Min, Kyung Hoon.
Afiliación
  • Park EJ; Hanmi Research Center, Hanmi Pharm. Co. Ltd, Gyeonggi-do 445-813, Republic of Korea; College of Pharmacy, Chung-Ang University, Seoul 156-756, Republic of Korea.
  • Ahn YG; Hanmi Research Center, Hanmi Pharm. Co. Ltd, Gyeonggi-do 445-813, Republic of Korea.
  • Jung SH; Hanmi Research Center, Hanmi Pharm. Co. Ltd, Gyeonggi-do 445-813, Republic of Korea.
  • Bang HJ; Hanmi Research Center, Hanmi Pharm. Co. Ltd, Gyeonggi-do 445-813, Republic of Korea; College of Pharmacy, Chung-Ang University, Seoul 156-756, Republic of Korea.
  • Kim M; Hanmi Research Center, Hanmi Pharm. Co. Ltd, Gyeonggi-do 445-813, Republic of Korea; College of Pharmacy, Chung-Ang University, Seoul 156-756, Republic of Korea.
  • Hong DJ; Hanmi Research Center, Hanmi Pharm. Co. Ltd, Gyeonggi-do 445-813, Republic of Korea; College of Pharmacy, Chung-Ang University, Seoul 156-756, Republic of Korea.
  • Kim J; Hanmi Research Center, Hanmi Pharm. Co. Ltd, Gyeonggi-do 445-813, Republic of Korea.
  • Suh KH; Hanmi Research Center, Hanmi Pharm. Co. Ltd, Gyeonggi-do 445-813, Republic of Korea.
  • Kim YJ; College of Pharmacy, Chung-Ang University, Seoul 156-756, Republic of Korea.
  • Kim D; College of Pharmacy, Chung-Ang University, Seoul 156-756, Republic of Korea.
  • Kim EY; College of Pharmacy, Korea University, Sejong 339-700, Republic of Korea.
  • Lee K; College of Pharmacy, Korea University, Sejong 339-700, Republic of Korea.
  • Min KH; College of Pharmacy, Chung-Ang University, Seoul 156-756, Republic of Korea. Electronic address: khmin@cau.ac.kr.
Bioorg Med Chem Lett ; 24(17): 4271-5, 2014 Sep 01.
Article en En | MEDLINE | ID: mdl-25082126
Takeda G-protein-coupled receptor 5 (TGR5) is a promising molecular target for metabolic diseases. A series of 4-(2,5-dichlorophenoxy)pyrimidine and cyclopropylmalonamide derivatives were synthesized as potent agonists of TGR5 based on a bioisosteric replacement strategy. Several compounds exhibited improved potency, compared to a reference compound with a pyridine scaffold. The pharmacokinetic profile of the representative compound 18 was considered moderate.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirimidinas / Sistema Enzimático del Citocromo P-450 / Receptores Acoplados a Proteínas G / Descubrimiento de Drogas / Inhibidores Enzimáticos del Citocromo P-450 / Malonatos Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2014 Tipo del documento: Article Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirimidinas / Sistema Enzimático del Citocromo P-450 / Receptores Acoplados a Proteínas G / Descubrimiento de Drogas / Inhibidores Enzimáticos del Citocromo P-450 / Malonatos Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2014 Tipo del documento: Article Pais de publicación: Reino Unido