title: Substituted dithiazole piperazine benzamides as novel amyloid beta peptide reducing agents.
abstract: Alzheimer's disease is a persistent neurodegenerative disorder of elderly characterized clinically by irreversible loss of memory due to accumulation of amyloid beta peptides within the amyloid plaques. We report the parallel synthesis and screening results of diverse substituted di-thiazole piperazine benzamides. A new compound TPI-1917-49 was identified as a promising amyloid reducing agent by lowering the levels of Aβ at least in two cell types and in vivo.
authors.affiliation: Torrey Pines Institute for Molecular Studies, Port Saint Lucie, FL 34987, United States.
authors.forename: Hongjie
authors.initials: H
authors.lastname: Wang
authors.affiliation: Torrey Pines Institute for Molecular Studies, Port Saint Lucie, FL 34987, United States.
authors.forename: Ruizhi
authors.initials: R
authors.lastname: Wang
authors.affiliation: Torrey Pines Institute for Molecular Studies, Port Saint Lucie, FL 34987, United States.
authors.forename: Madepalli K
authors.initials: MK
authors.lastname: Lakshmana
authors.affiliation: Torrey Pines Institute for Molecular Studies, Port Saint Lucie, FL 34987, United States. Electronic address: adeln@tpims.org.
authors.forename: Adel
authors.initials: A
authors.lastname: Nefzi
mesh_terms: D016229:Amyloid beta-Peptides / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000818:Animals; D001549:Benzamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D016466:CHO Cells; D016923:Cell Death / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003412:Cricetulus; D004305:Dose-Response Relationship, Drug; D051379:Mice; D008968:Molecular Conformation; D010084:Oxidation-Reduction / Q000187:drug effects; D000077489:Piperazine; D010879:Piperazines / Q000737:chemistry*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000737:chemistry*
chemical_list: D016229:Amyloid beta-Peptides; D001549:Benzamides; D010879:Piperazines; D013844:Thiazoles; D000077489:Piperazine
keywords: Alzheimer’s disease; Amyloid reducing agent; Parallel synthesis; Thiazole