4.7 Article

Macrocyclic BACE1 inhibitors with hydrophobic cross-linked structures: Optimization of ring size and ring structure

相关参考文献

注意:仅列出部分参考文献,下载原文获取全部文献信息。
Article Biochemistry & Molecular Biology

Structure-activity relationship study of hydroxyethylamine isostere and P1′ site structure of peptide mimetic BACE1 inhibitors

Kazuya Kobayashi et al.

Summary: The introduction of an aromatic substituent into a HEA-type BACE1 inhibitor enhanced inhibitory activity, with the R-configuration improving activity and methyl substitution decreasing activity. Isosteres with different hydroxyl and methyl configurations were prepared using a branched synthesis approach, and the effect on inhibitory activity was evaluated. Derivatives with various substituents at the P1' site showed clear effects on BACE1 activity, leading to the identification of a highly potent inhibitor.

BIOORGANIC & MEDICINAL CHEMISTRY (2021)

Review Chemistry, Medicinal

New evolutions in the BACE1 inhibitor field from 2014 to 2018

Chien-Chi Hsiao et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2019)

Article Chemistry, Organic

A Motif-Oriented Total Synthesis of Nannocystin Ax. Preparation and Biological Assessment of Analogues

Zhanchao Meng et al.

JOURNAL OF ORGANIC CHEMISTRY (2018)

Article Medicine, General & Internal

Randomized Trial of Verubecestat for Mild-to-Moderate Alzheimer's Disease

Michael F. Egan et al.

NEW ENGLAND JOURNAL OF MEDICINE (2018)

Review Biochemistry & Molecular Biology

Development and Structural Modification of BACE1 Inhibitors

Ting Gu et al.

MOLECULES (2017)

Article Chemistry, Organic

Carbon-Phosphorus Bond Formation on Anilines Mediated by a Hypervalent Iodine Reagent

Elsa Deruer et al.

JOURNAL OF ORGANIC CHEMISTRY (2017)

Article Biochemistry & Molecular Biology

Evaluation of transition-state mimics in a superior BACE1 cleavage sequence as peptide-mimetic BACE1 inhibitors

Yasunao Hattori et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2015)

Review Chemistry, Multidisciplinary

BACE1 (beta-secretase) inhibitors for the treatment of Alzheimer's disease

Arun K. Ghosh et al.

CHEMICAL SOCIETY REVIEWS (2014)

Article Chemistry, Medicinal

Macrocyclic Drugs and Clinical Candidates: What Can Medicinal Chemists Learn from Their Properties?

Fabrizio Giordanetto et al.

JOURNAL OF MEDICINAL CHEMISTRY (2014)

Article Chemistry, Medicinal

Hydroxyethylamine-based inhibitors of BACE1: P1-P3 macrocyclization can improve potency, selectivity, and cell activity

Lewis D. Pennington et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2013)

Article Biochemistry & Molecular Biology

Evaluation of superior BACE1 cleavage sequences containing unnatural amino acids

Taeko Kakizawa et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2011)

Article Chemistry, Inorganic & Nuclear

Efficient synthesis of benzyl 2-(S)-[(tert-butoxycarbonyl)amino]-ω-iodoalkanoates

Yohei Koseki et al.

TETRAHEDRON-ASYMMETRY (2011)

Article Chemistry, Medicinal

Potent and Fully Noncompetitive Peptidomimetic Inhibitor of Multidrug Resistance P-Glycoprotein

Ophelie Arnaud et al.

JOURNAL OF MEDICINAL CHEMISTRY (2010)

Article Chemistry, Medicinal

Prolonged stability by cyclization: Macrocyclic phosphino dipeptide isostere inhibitors of β-secretase (BACE1)

Timo Huber et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2009)

Article Biochemistry & Molecular Biology

Conformationally constrained mimics of the membrane-proximal domain of FcεRIα

Carsten Peters et al.

CHEMBIOCHEM (2007)

Article Chemistry, Organic

A general strategy for the synthesis of azapeptidomimetic lactams

RL Broadrup et al.

TETRAHEDRON (2005)

Review Physiology

Alzheimer's disease: Genes, proteins, and therapy

DJ Selkoe

PHYSIOLOGICAL REVIEWS (2001)