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Tuesday, August 4, 2020 | History

2 edition of Synthesis of novel inositol derivatives as amyloid inhibitors found in the catalog.

Synthesis of novel inositol derivatives as amyloid inhibitors

Yedi Sun

Synthesis of novel inositol derivatives as amyloid inhibitors

by Yedi Sun

  • 334 Want to read
  • 13 Currently reading

Published .
Written in English


Edition Notes

ContributionsUniversity of Toronto. Dept. of Chemistry.
The Physical Object
Paginationviii, 89 leaves :
Number of Pages89
ID Numbers
Open LibraryOL20893554M

A stereoisomer of inositol, scyllo-inositol, is known as a promising therapeutic agent for Alzheimer's disease, since it prevents the accumulation of beta-amyloid deposits, a hallmark of the ://   Title:Identification of Novel BACE1 Inhibitors by Combination of Pharmacophore Modeling, Structure-Based Design and In Vitro Assay VOLUME: 12 ISSUE: 1 Author(s):Yuan Ju, Zicheng Li, Yong Deng, Aiping Tong, Liangxue Zhou and Youfu Luo Affiliation:State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center for

Alzheimer’s disease (AD) is the most prevalent neurodegenerative disorder worldwide. Currently, the only strategy for palliative treatment of AD is to inhibit acetylcholinesterase (AChE) in order to increase the concentration of acetylcholine in the synaptic cleft. Evidence indicates that AChE also interacts with the β-amyloid (Aβ) protein, acting as a chaperone and increasing the number   Title:Design, Synthesis and Biological Evaluation of Some Oxadiazole Derivatives as Novel Amide-Based Inhibitors of Soluble Epoxide Hydrolase VOLUME: 11 ISSUE: 6 Author(s):Elham Rezaee Zavareh, Mahdi Hedayati, Laleh Hoghooghi Rad, Azin Kiani, Soraya Shahhosseini, Mehrdad Faizi and Sayyed Abbas Tabatabai Affiliation:Department of Pharmaceutical Chemistry, School of Pharmacy, ?genre.

A series of benzofuran derivatives were designed and synthesized, and their inhibitory activites were measured against the SIRT1–3. The enzymatic assay showed that all the compounds showed certain anti-SIRT2 activity and selective over SIRT1 and SIRT3 with IC50 (half maximal inhibitory concentration) values at the micromolar level. The preliminary structure–activity relationships were Synthesis and Biological Evaluation as Glycosidase Inhibitors. Article in Bioorganic & Medicinal Chemistry Letters 14(5) April with 15 Reads How we measure 'reads'


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Synthesis of novel inositol derivatives as amyloid inhibitors by Yedi Sun Download PDF EPUB FB2

Divergent Synthesis of scyllo-Inositol Aldoxime Derivatives as Potential Inhibitors of Amyloid-Beta() Aggregate Formation Jason Song Ngai Chio Master of Sciences Graduate Department of Chemistry University of Toronto Abstract scyllo-Inositol is currently in phase II clinical trials as a therapeutic for Alzheimer’s disease (AD).

1. Eur J Med Chem. Oct 15; doi: / Epub Jul Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's ://   Divergent Synthesis of scyllo-Inositol Aldoxime Derivatives as Potential Inhibitors of Amyloid-Beta() Aggregate Formation; Author: Chio, Subsequent oxime formation with aromatic aldehydes generated a novel class of inositol derivatives in good yield and high purity.

The effects of these compounds on the Ab aggregation cascade were scyllo-Inositol has shown promise as a potential therapeutic for Alzheimer’s disease, by directly interacting with the amyloid β (Aβ) peptide to inhibit Aβ42 fiber explore the molecular details of the inositol-Aβ42 Synthesis of novel inositol derivatives as amyloid inhibitors book, a series of scyllo-inositol derivatives have been synthesized which contain deoxy, fluoro, chloro, and methoxy ://   Synthesis of scyllo-inositol derivatives and their effects on amyloid beta peptide aggregation.

Bioorganic & Medicinal Chemistry16 (15), DOI: / Junghun Suh, Woo Suk Chei, Tae Yeon Lee, Min Gyum Kim, Sang Ho Yoo, Keunhong Jeong, Jae Young :// The novel imidazo[1,2-a]pyridine derivatives were synthesized from bromoketone 1 as shown in Scheme sis of 2 bearing imidazo[1,2-a]pyridine skeleton was achieved by reaction of bromoketone 1 with 2-aminopyridines under mild basic conditions.

The cyano derivative 2 was used as a common intermediate in the synthesis of DRM, DRK, DRM, and DRM SH2 domain-containing inositol 5′-phosphatase 2 (SHIP2) is a lipid phosphatase that produce phosphatidylinositol 3,4-bisphosphate (PI(3,4)P 2) from phosphatidylinositol 3,4,5-triphosphate (PI(3,4,5)P 3), and is involved in many diseases such as neurodegenerative diseases.A recent report demonstrating that SHIP2 inhibition decreased tau hyperphosphorylation induced by amyloid β and   Islet amyloid polypeptide (IAPP, amylin) is responsible for amyloid formation in type 2 diabetes and in transplanted islets.

The flavanol (−)-epigallocatechingallate [EGCG; (2R,3R)-5,7-dihydroxy(3,4,5-trihydroxyphenyl)-3,4-dihydro-2Hbenzopyranyl 3,4,5-trihydroxybenzoate] is an effective inhibitor of amyloid formation by IAPP; however, the interactions required for the inhibition   Gaining insight into the mechanism of amyloid fibril formation, the hallmark of multiple degenerative syndromes of unrelated origin, and exploring novel directions of inhibition are crucial for preventing disease development.

Specific interactions between aromatic moieties were suggested to have a key role in the recognition and self-assembly processes leading to the formation of amyloid Synthesis of Best-Seller Drugs is a key reference guide for all those involved with the design, development, and use of the best-selling drugs.

Designed for ease of use, this book provides detailed information on the most popular drugs, using a practical layout arranged according to drug ://   Lalut, J., Payan, H., Davis, A.

et al. Rational design of novel benzisoxazole derivatives with acetylcholinesterase inhibitory and serotoninergic 5-HT 4 receptors activities for the treatment of   Assessment of Novel Curcumin Derivatives as Potent Inhibitors of Inflammation and Amyloid-β Aggregation in Alzheimer’s Disease Synthesis of curcumin derivatives with ether, ester, and diesther groups.

Reagents and conditions: a) CHCCH 2 Br, K 2 CO 3, DMF, RT, 48 h, 70%. Aβ Fragments or Aβ Derivatives. Self-aggregation is a predominant characteristic of amyloid proteins.

An attractive strategy for developing amyloid aggregation inhibitors is to use fragments of the wild-type peptide, particularly those derived from sequences known to mediate aggregation because of their known tendency to ://   Title:Design, Synthesis and Characterization of Novel Urolithin Derivatives as Cholinesterase Inhibitor Agents VOLUME: 15 ISSUE: 11 Author(s):Maryam Norouzbahari, Emine V.

Burgaz, Tugba Ercetin, Amirhossein Fallah, Alireza Foroumadi, Loghman Firoozpour, Mustafa F. Sahin, Mustafa Gazi and Hayrettin O. Gulcan* Affiliation:Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Divergent synthesis of biflavonoids yields novel inhibitors of the aggregation of amyloid β (1–42)† Tze Han Sum, a Tze Jing Sum, a Súil Collins, ab Warren R.

Galloway, a David G. Twigg, a Florian Hollfelder b and David R. Spring * a   Aggregation of Aβ42 and formation of amyloid plaques is considered one of the important pathological events in AD.

1 A number of potential therapeutic compounds have been developed as inhibitors of Aβ42 aggregation. 2,3 To determine if IAM1 also acts as an inhibitor of Aβ42 aggregation, we applied an in situ kinetic thioflavin T (ThT) assay. 47−49 This assay is based on increase in ThT   The design and application of an effective, new class of organofluorine inhibitors of amyloid fibrillogenesis are described.

Based on experimental evidence a core structure containing indolyl, trifluoromethyl, hydroxyl, and carboxylic acid ester functions has been designed. Several substituted derivatives of this core structure have been synthesized, using various indole ://   Many compounds have been tested as inhibitors or modulators of amyloid β-protein (Aβ) assembly in hope that they would lead to effective, disease-modifying therapy for Alzheimer’s disease (AD).

These compounds typically were either designed to break apart β-sheets or selected empirically. Two such compounds, the natural inositol derivative scyllo-inositol and the green-tea-derived   Identification of crizotinib derivatives as potent SHIP2 inhibitors for the treatment of Alzheimer's disease.

SH2 domain-containing inositol 5'-phosphatase 2 (SHIP2) is a lipid phosphatase that produce phosphatidylinositol 3,4-bisphosphate (PI(3,4)P2) from phosphatidylinositol 3,4,5-triphosphate (PI(3,4,5)P3), and is involved in many   Another novel compound scyllo-cyclohexanehexol (AZD, ELND), a blood-brain barrier permeable stereoisomer of inositol which binds and arrests Aβ aggregation has displayed promising activity in animal studies in reducing Aβ40 and Aβ42 load, inflammation and restoring synaptic loss and improving ://.

Notably, stabilization of non-toxic oligomers appears to be a general mechanism for inhibitors of Aβ assembly and toxicity, including scyllo-inositol, 46 epigallocatechin gallate, 43 resveratrol 47 and other polyphenols, 48 and peptides derived from the C-terminus of Aβ 49,50 If this mechanism is found to be applicable to other Molecular docking simulation, synthesis and 3D pharmacophore studies of novel 2-substitutednitro-benzimidazole derivatives as anticancer agents targeting VEGFR-2 and c-Met Heba A.

Ibrahim, Fadi M. Awadallah, Hanan M. Refaat, Kamilia M. Amin  Amyloid β (Aβ) peptides have long been viewed as a potential target for Alzheimer's disease (AD).

Aggregation of Aβ peptides in the brain tissue is believed to be an exclusively pathological