Synthesis and structure-activity relationship of a novel series of heterocyclic sulfonamide gamma-secretase inhibitors

Autor:	Joshua D Berkowitz, Boyd L. Harrison, Robert Martone, Hua Zhou, Micheal Chlenov, Yun Hu, Peimin Lu, Koi Michele Morris, June Sonnenberg-Reines, S. Aschmies, Joan E. Sabalski, Kerri Lipinski, George Diamantidis, Kevin Atchison, Thomas J. Caggiano, Shaiu-Ching Sun, Zheng Xu, Jun Pu, Anthony F. Kreft, Dave R. Riddell, Yiqun Wang, Lynn Resnick, Mei Jin, Donna M. Huryn, Erik Wagner, J. Steven Jacobsen
Rok vydání:	2009
Předmět:	Stereochemistry Clinical Biochemistry Pharmaceutical Science CHO Cells Biochemistry Chemical synthesis Structure-Activity Relationship Cricetulus Alzheimer Disease Heterocyclic Compounds Cricetinae Drug Discovery medicine Amyloid precursor protein Structure–activity relationship Animals Humans Molecular Biology chemistry.chemical_classification Sulfonamides Amyloid beta-Peptides biology Molecular Structure Receptors Notch Organic Chemistry medicine.disease Sulfonamide Enzyme chemistry Enzyme inhibitor biology.protein Molecular Medicine Alzheimer's disease Amyloid Precursor Protein Secretases Amyloid precursor protein secretase Protein Binding
Zdroj:	Bioorganicmedicinal chemistry. 17(13)
ISSN:	1464-3391
Popis:	gamma-Secretase inhibitors have been shown to reduce the production of beta-amyloid, a component of the plaques that are found in brains of patients with Alzheimer's disease. A novel series of heterocyclic sulfonamide gamma-secretase inhibitors that reduce beta-amyloid levels in cells is reported. Several examples of compounds within this series demonstrate a higher propensity to inhibit the processing of amyloid precursor protein compared to Notch, an alternative gamma-secretase substrate.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ccb35335c5e137415c463df8839ade10 https://pubmed.ncbi.nlm.nih.gov/19443228 Zobrazit plný text záznamu Full Text from ScienceDirect