Synthesis and optimization of picolinamide derivatives as a novel class of 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1) inhibitors.

Ryu, Je Ho; Kim, Shinae; Lee, Jung A; Han, Hye Young; Son, Hyun Joo; Lee, Hyun Jung; Kim, Yong Hyuk; Kim, Jae-Sun; Park, Hyeung-Geun

Ryu, Je Ho; Kim, Shinae; Lee, Jung A; Han, Hye Young; Son, Hyun Joo; Lee, Hyun Jung; Kim, Yong Hyuk; Kim, Jae-Sun; Park, Hyeung-Geun.

Afiliação

Ryu JH; Life Science R&D Center, SK Chemicals, 686 Sampyeong-dong, Bundang-gu, Seongnam-si 463-400, Republic of Korea; Research Institute of Pharmaceutical Science and College of Pharmacy, Seoul National University, Seoul 151-742, Republic of Korea.
Kim S; Life Science R&D Center, SK Chemicals, 686 Sampyeong-dong, Bundang-gu, Seongnam-si 463-400, Republic of Korea.
Lee JA; Life Science R&D Center, SK Chemicals, 686 Sampyeong-dong, Bundang-gu, Seongnam-si 463-400, Republic of Korea.
Han HY; Life Science R&D Center, SK Chemicals, 686 Sampyeong-dong, Bundang-gu, Seongnam-si 463-400, Republic of Korea.
Son HJ; Life Science R&D Center, SK Chemicals, 686 Sampyeong-dong, Bundang-gu, Seongnam-si 463-400, Republic of Korea.
Lee HJ; Life Science R&D Center, SK Chemicals, 686 Sampyeong-dong, Bundang-gu, Seongnam-si 463-400, Republic of Korea.
Kim YH; Life Science R&D Center, SK Chemicals, 686 Sampyeong-dong, Bundang-gu, Seongnam-si 463-400, Republic of Korea.
Kim JS; Life Science R&D Center, SK Chemicals, 686 Sampyeong-dong, Bundang-gu, Seongnam-si 463-400, Republic of Korea.
Park HG; Research Institute of Pharmaceutical Science and College of Pharmacy, Seoul National University, Seoul 151-742, Republic of Korea. Electronic address: hgpk@snu.ac.kr.

Bioorg Med Chem Lett ; 25(8): 1679-1683, 2015 Apr 15.

Article em En | MEDLINE | ID: mdl-25800116

Assuntos

11-beta-Hidroxiesteroide Desidrogenase Tipo 1/metabolismo; Inibidores Enzimáticos/síntese química; Ácidos Picolínicos/química; 11-beta-Hidroxiesteroide Desidrogenase Tipo 1/antagonistas & inibidores; Administração Oral; Amidas/química; Amidas/farmacocinética; Amidas/uso terapêutico; Animais; Glicemia/análise; Catálise; Diabetes Mellitus Experimental/tratamento farmacológico; Inibidores Enzimáticos/farmacocinética; Inibidores Enzimáticos/uso terapêutico; Células HEK293; Meia-Vida; Humanos; Lipídeos/sangue; Masculino; Camundongos; Camundongos Endogâmicos C57BL; Camundongos Obesos; Paládio/química; Ácidos Picolínicos/farmacocinética; Ácidos Picolínicos/uso terapêutico; Ligação Proteica; Relação Estrutura-Atividade

Palavras-chave

11ß-HSD1 inhibitor; Diabetes; Hyperlipidemia; Metabolic syndrome; Picolinamide

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Ácidos Picolínicos / 11-beta-Hidroxiesteroide Desidrogenase Tipo 1 / Inibidores Enzimáticos Idioma: En Ano de publicação: 2015 Tipo de documento: Article

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