Discovery and optimization of novel 3-benzyl-N-phenyl-1H-pyrazole-5-carboxamides as bifunctional antidiabetic agents stimulating both insulin secretion and glucose uptake.

Jo, Jeyun; Lee, Dahae; Park, Yeong Hye; Choi, Hyeonjin; Han, Jinhee; Park, Do Hwi; Choi, You-Kyung; Kwak, Jinsook; Yang, Min-Kyu; Yoo, Jin-Wook; Moon, Hyung Ryong; Geum, Dongho; Kang, Ki Sung; Yun, Hwayoung

Jo, Jeyun; Lee, Dahae; Park, Yeong Hye; Choi, Hyeonjin; Han, Jinhee; Park, Do Hwi; Choi, You-Kyung; Kwak, Jinsook; Yang, Min-Kyu; Yoo, Jin-Wook; Moon, Hyung Ryong; Geum, Dongho; Kang, Ki Sung; Yun, Hwayoung.

Afiliación

Jo J; College of Pharmacy, Pusan National University, Busan, 46241, Republic of Korea.
Lee D; College of Korean Medicine, Gachon University, Seongnam, 13120, Republic of Korea.
Park YH; College of Pharmacy, Pusan National University, Busan, 46241, Republic of Korea.
Choi H; College of Pharmacy, Pusan National University, Busan, 46241, Republic of Korea.
Han J; College of Pharmacy, Pusan National University, Busan, 46241, Republic of Korea.
Park DH; College of Korean Medicine, Gachon University, Seongnam, 13120, Republic of Korea.
Choi YK; College of Korean Medicine, Gachon University, Seongnam, 13120, Republic of Korea.
Kwak J; College of Pharmacy, Pusan National University, Busan, 46241, Republic of Korea.
Yang MK; Mother's Pharmaceutical, Seoul, 08506, Republic of Korea.
Yoo JW; College of Pharmacy, Pusan National University, Busan, 46241, Republic of Korea.
Moon HR; College of Pharmacy, Pusan National University, Busan, 46241, Republic of Korea.
Geum D; Department of Biomedical Sciences, Korea University Medical School, Seoul, 02841, Republic of Korea.
Kang KS; College of Korean Medicine, Gachon University, Seongnam, 13120, Republic of Korea. Electronic address: kkang@gachon.ac.kr.
Yun H; College of Pharmacy, Pusan National University, Busan, 46241, Republic of Korea. Electronic address: hyun@pusan.ac.kr.

Eur J Med Chem ; 217: 113325, 2021 May 05.

Article en En | MEDLINE | ID: mdl-33765605

Asunto(s)

Descubrimiento de Drogas; Glucosa/metabolismo; Hipoglucemiantes/farmacología; Insulina/metabolismo; Pirazoles/farmacología; Supervivencia Celular/efectos de los fármacos; Células Cultivadas; Relación Dosis-Respuesta a Droga; Humanos; Hipoglucemiantes/síntesis química; Hipoglucemiantes/química; Estructura Molecular; Pirazoles/síntesis química; Pirazoles/química; Relación Estructura-Actividad; Proteínas de Motivos Tripartitos/antagonistas & inhibidores; Proteínas de Motivos Tripartitos/metabolismo

Palabras clave

3-Benzyl-N-phenyl-1H-pyrazole-5-carboxamide; Glucose stimulation index (GSI); Glucose-stimulated insulin secretion (GSIS); Structure-activity relationship (SAR); Type 2 diabetes mellitus (T2DM)

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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Pirazoles / Descubrimiento de Drogas / Glucosa / Hipoglucemiantes / Insulina Tipo de estudio: Prognostic_studies Límite: Humans Idioma: En Revista: Eur J Med Chem Año: 2021 Tipo del documento: Article

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