4-Substituted 2-amino-3,4-dihydroquinazolines with a 3-hairpin turn side chain as novel inhibitors of BACE-1.

Jagtap, Ajit Dhananjay; Kondekar, Nagendra B; Hung, Pei-Yun; Hsieh, Chen-En; Yang, Chia-Ron; Chen, Grace Shiahuy; Chern, Ji-Wang

Jagtap, Ajit Dhananjay; Kondekar, Nagendra B; Hung, Pei-Yun; Hsieh, Chen-En; Yang, Chia-Ron; Chen, Grace Shiahuy; Chern, Ji-Wang.

Afiliación

Jagtap AD; School of Pharmacy, College of Medicine and Center for Innovative Therapeutics Discovery, National Taiwan University, No. 33, Lin Sen South Road, Taipei 10050, Taiwan; AnnJi Pharmaceutical Co., Ltd., 18, Siyuan Street, Taipei 10087, Taiwan.
Kondekar NB; School of Pharmacy, College of Medicine and Center for Innovative Therapeutics Discovery, National Taiwan University, No. 33, Lin Sen South Road, Taipei 10050, Taiwan.
Hung PY; AnnJi Pharmaceutical Co., Ltd., 18, Siyuan Street, Taipei 10087, Taiwan.
Hsieh CE; Department of Applied Chemistry, Providence University, No. 200, Section 7, Taiwan Boulevard, Taichung 43301, Taiwan.
Yang CR; School of Pharmacy, College of Medicine and Center for Innovative Therapeutics Discovery, National Taiwan University, No. 33, Lin Sen South Road, Taipei 10050, Taiwan.
Chen GS; Department of Applied Chemistry, Providence University, No. 200, Section 7, Taiwan Boulevard, Taichung 43301, Taiwan. Electronic address: grace@pu.edu.tw.
Chern JW; School of Pharmacy, College of Medicine and Center for Innovative Therapeutics Discovery, National Taiwan University, No. 33, Lin Sen South Road, Taipei 10050, Taiwan. Electronic address: jwchern@ntu.edu.tw.

Bioorg Chem ; 95: 103135, 2020 01.

Article en En | MEDLINE | ID: mdl-31923631

Asunto(s)

Secretasas de la Proteína Precursora del Amiloide/antagonistas & inhibidores; Ácido Aspártico Endopeptidasas/antagonistas & inhibidores; Inhibidores Enzimáticos/farmacología; Secretasas de la Proteína Precursora del Amiloide/metabolismo; Ácido Aspártico Endopeptidasas/metabolismo; Línea Celular Tumoral; Relación Dosis-Respuesta a Droga; Inhibidores Enzimáticos/síntesis química; Inhibidores Enzimáticos/química; Humanos; Modelos Moleculares; Conformación Molecular; Quinazolinas/síntesis química; Quinazolinas/farmacología; Relación Estructura-Actividad

Palabras clave

2-amino-3; 4-dihydroquinazolines; Alzheimer's disease; BACE-1; Non-peptidic aspartyl protease inhibitors; Structure-activity relationship

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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Ácido Aspártico Endopeptidasas / Inhibidores Enzimáticos / Secretasas de la Proteína Precursora del Amiloide Límite: Humans Idioma: En Revista: Bioorg Chem Año: 2020 Tipo del documento: Article País de afiliación: Taiwán

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