Phenyl(cyclo)alkylamines : Second generation P_1' position analogs for pentapeptidic BACE1 inhibitors

スポンサーリンク

概要

• 論文の詳細を見る
• 2011-03-01

著者

• Kiso Y

  Department Of Medicinal Chemistry Kyoto Pharmaceutical University

• 木村 富美夫

  Pharmaceutical Research Department Ube Laboratory Corporate Research & Development Ube Industrie

• HAMADA Yoshio

  Department of Medicinal Chemistry, Center for Frontier Research in Medicinal Science, 21st Century C

• Hidaka Koushi

  Department Of Medicinal Chemistry Center For Frontier Research In Medicinal Science 21st Century Coe

• Hayashi Yoshio

  Department Of Medicinal Chemistry Kyoto Pharmaceutical University

• Kinoshita Yuko

  Department Of Oriental Medicine Nihon University School Of Medicine

• Kimura Tomio

  Pharmaceutical Research Department Ube Laboratory Corporate Research & Development Ube Industrie

• 景山 節

  京都大学霊長類研究所人類進化モデル研究センター

• Kimura T

  Department Of Medicinal Chemistry Center For Frontier Research In Medicinal Science 21st Century Coe

• Sohma Youhei

  Department Of Medicinal Chemistry Center For Frontier Research In Medicinal Science 21st Century Coe

• Kimura Tooru

  Department Of Medicinal Chemistry Kyoto Pharmaceutical University

• Kiso Yoshiaki

  Department Of Medicinal Chemistry Center For Frontier Research In Medicinal Science 21st Century Coe

• Kiso Yoshiaki

  21st Century Coe Program Kyoto Pharmaceutical University

• Hidaka Koushi

  Department Of Medicinal Cemistry Center For Frontier Research In Medicinal Science 21st Century Coe

• Kiso Yoshiaki

  Kyoto Pharmaceutical Univ. Kyoto Jpn

• Hayashi Yoshio

  Department Of Electrical And Electronic Engineering Kitami Institute Of Technology

• Kiso Yoshiaki

  Protein Research Group Riken Genomic Sciences Center

• Yamaguchi H

  Department Of Oral Molecular Pathology Institute Of Health Bioscience The University Of Tokushima Gr

• Kimura Tooru

  Department Of Medicinal Chemistry Center For Frontier Research In Medicinal Science Kyoto Pharmaceut

• TAGAD Harichandra

  Department of Medicinal Chemistry, Center for Frontier Research in Medicinal Science, Kyoto Pharmace

• Tagad Harichandra

  Department Of Medicinal Chemistry Center For Frontier Research In Medicinal Science Kyoto Pharmaceut

• Hayashi Yoshio

  Department Of Medicinal Chemistry Center For Frontier Research In Medicinal Science Kyoto Pharmaceut

• Kimura T

  Peptide Inst. Inc. Minoh Jpn

• KISO Yoshiaki

  Department of Ecological Engineering, Toyohashi University of Technology, JAPAN.

• HAMADA Yoshio

  Department of Cardiovascular Surgery and Internal Medicine, Saiseikai Shimonoseki General Hospital

関連論文

• カンナビノイドの代謝的活性化とシトクロムP450分子種
• Butyrylcholinesterase and Erythrocyte Sulfhydryl-dependent Enzyme Hydrolyze Gabexate in Human Blood
• Involvement of Human Blood Arylesterases and Liver Microsomal Carboxylesterases in Nafamostat Hydrolysis
• Development of New Photoresponsive Paclitaxel Prodrug
• Phototaxel : Development of First Photoresponsive Prodrug of Paclitaxel via Modification of Phenylisoserine Moiety
• "Click Peptide" : the "O-Acyl Isopeptide Method" for Peptide Synthesis and Development of Chemical Biology-Oriented Aβ Analogues
• "Click Peptide" Based on the "O-Acyl Isopeptide Method" : Development of Chemical Biology-Oriented Alzheimer's Disease-Related Aβ1-42 Analogues
• サル腎ミクロソームによるTetrahydrocannabinolの代謝
• Design and Synthesis of Dipeptide-type HIV-1 Protease Inhibitors with High Antiviral Activity
• New Type Prodrugs of Anti-HIV Agents Consisting of the HIV Protease Inhibitor and Reverse Transcriptase Inhibitor
• Synthesis and Activity of a New Type of Anti-HIV Agents, Conjugate of HIV Protease Inhibitor with Reverse Transcriptase Inhibitor
• Synthesis of an HIV-1 Protease Analogue by the Chemoselective Ligation Method Using a New Disulfide Type Linker
• Racemization-Free Segment Condensation Based on Isopeptide Method : An Efficient Preparation of Peptides on Solid Support
• The Synthesis of Bioactive Peptides Based on O-Acyl Isopeptide Method : Application of O-Acyl Isodipeptide Units
• Development of Racemization-Free "O-Acyl Isopeptide Method" Utilizing the "O-Acyl Isodipeptide Unit"
• P-262 "O-ACYL ISOPEPTIDE METHOD" FOR THE EFFICIENT SYNTHESIS OF DIFFICULT SEQUENSE-CONTAINING PEPTIDES : UTILIZATION OF "O-ACYL ISODIPEPTIDE UNIT"
• Conversion of Polymer-Bound Dipeptide to Evans-Type Chiral Auxiliary : A New Tool for Efficient Solid-Phase Asymmetric Reactions
• Structure-Activity Relationship of Orally Potent Tripeptide-Based HIV Protease Inhibitors Containing Hydroxymethylcarbonyl Isostere
• Small-sized HIV Protease Inhibitors Containing Allophenylnorstatine as a Substrate Transition-state Mimic
• Design of HIV Protease Inhibitors Based on the Transition State Analogue Concept
• Novel 2-Amino-1,4-dihydropyridine Calcium Antagonists. II. Synthesis and Antihypertensive Effects of 2-Amino-1,4-dihydropyridine Derivatives Having N, N-Dialkylaminoalkoxycarbonyl Groups at 3- and/or 5-Position
• Novel 2-Amino-1,4-dihydropyridine Calcium Antagonists. I. Synthesis and Antihypertensive Effects of 2-Amino-1,4-dihydropyridine Derivatives Having Nitroxyalkoxycarbonyl Groups at 3- and/or 5-Position
• Novel BACE1 Inhibitors : Design Approach Focused on Inhibitor's Conformer
• Structure-Activity Relationship Study of BACE1 Inhibitors Containing Chelidonamide
• Synthesis of HIV Protease Dipeptide Inhibitors and Prodrugs
• Oligoarginine-Based Prodrugs with Self-Cleavable Spacers for Caco-2 Cell Permeation
• Synthesis and Activity of Tetrapeptidic Human T-cell Leukemia Virus Type I Protease Inhibitors Possessing Different P_1'- and P_3-cap Moieties
• Design of BACE1 Inhibitors : Replacing the P_1' Residue with Non-Acidic Moiety
• Design and Synthesis of Conformationally Constrained Dimerization Inhibitors of HIV-1 Protease
• Synthesis of Negamycin and Its Derivatives as Potential Therapeutic Agents for Duchenne Muscular Dystrophy
• Structural Analysis of Amyloid-β Protein Fibrils Formed in Raft-Like Model Membranes
• Inhibition of Amyloid β-Protein Aβ-(1-42) Induced Cytotoxicity by Helical Aβ Analog
• Phenylthionorstatine as a Transition-State Mimic in BACE1 Inhibitors
• Tripeptide Mimetics with Potent Inhibitory Activity against Malarial Aspartic Protease Plasmepsin II
• P-296 DEVELOPMENT OF RESIN SUPPORTED EVANS-TYPE CHIRAL AUXILIARY FOR SOLID-PHASE ASYMMETRIC REACTION
• Modification of P4 Position in β-secretase (BACE1) Inhibitors Containing Phenylnorstatine
• Design of β-Secretase (BACE1) Inhibitors with Carboxylic Acid Bioisosteres
• Evaluation of Peptidomimetic HTLV-I Protease Inhibitors Containing Hydroxymethylcarbonyl as a Transition-State Isostere
• O-N Intramolecular Acyloxy Migration Reaction : from the Prodrug Strategy to the Migration of Protective Groups in Amino Acids
• "Click Peptide" Based on the "O-Acyl Isopeptide Method" : an Efficient Preparation of Amyloid β Peptide 1-42 Mutants
• Design and Synthesis of β-Secretase Inhibitors Containing Hydroxymethylcarbonyl Isostere as a Transition State Mimic
• SYNTHESES AND STRUCTURE-ACTIVITY RELATIONSHIPS OF ATRIAL NATRIURETIC PEPTIDE (ANP) DERIVATIVES
• High-throughput Screening Method for Ligand Peptides Using Capillary Electrophoresis-Mass Spectrometry (CE-MS)
• A Novel S-Acyl Isopeptide Method for the Synthesis of Difficult Sequence-Containing Peptide
• Isopeptide Method : A Racemization-Free Peptide Synthesis by Segment Condensation
• Design and Synthesis of Inhibitory Peptides against EGF Receptor Dimerization
• SAR study of BACE1 inhibitors containing pyridine derivatives
• Significance of interaction of BACE1-Arg235 with its ligands and design of BACE1 inhibitors
• Chemical Synthesis of 71-meric Neuregulin 1-β1
• Click Peptide by Use of the O-Acyl Isopeptide Method : Production of Amyloid β Peptide from Water-Soluble Analogue
• "O-Acyl Isopeptide Method" for the Synthesis of Difficult Sequence-Containing Peptides : Application to the Synthesis of Amyloid β Peptide (Aβ) 1-42
• Development of Biotin-Tagged Tubulin Photoaffinity Probes Derivatized from Diketopiperazine Based Anti-Microtubule Agents
• Effect of the Phenyl Ring Modification on the Antitumor Activity of Anti-Microtubule Agent Dehydrophenylahistin
• Uptake Mechanisms of FITC-Oligoarginine Conjugates in HeLa Cells
• Design and Synthesis of Oligoarginine-Fluorescein Conjugates Possessing Novel Self-Cleavable Spacers as a Model for Effective Intestinal Absorption
• Efficient Total Synthesis of (+)-Negamycin and Its Derivatives
• Small Peptide-based Medicinal Chemistry for Intractable Disease
• A Synthetic Method for Monodehydro-Cyclic-Dipeptides toward Natural Product Synthesis
• New Aspects of Potent Anti-Microtubule Agents Phenylahistin and Tubulin Photoaffinity Labeling
• P-518 DEVELOPMENT OF POTENT ANTI-MICROTUBULE AGENTS BASED ON NATURAL DIKETOPIPERAZINE PHENYLAHISTIN AND TUBULIN PHOTOAFFINITY LABELING
• Development of a New Synthetic Method for Monodehydro-2,5-diketopiperazines
• Synthetic Study of Anti-microtubule Diketopiperazines : Phenylahistin and Aurantiamine
• Studies on N^〈in〉-Protecting Groups during the Synthesis of Trp : Containing Cystine Peptide by Silyl Chloride Sulfoxide Method
• A Reductive Acidolysis Final Deprotection Strategy in Solid Phase Peptide Synthesis Based on Safety-Catch Protection
• Effect of Dipeptidomimetics on Malaria Parasite Proliferation Inhibition Targeting Plasmepsin
• Design and Synthesis of Highly Active β-Secretase (BACE1) inhibitors, KMI-420 and KMI-429, with Enhanced Chemical Stability
• Evaluation of Peptidomimetic Inhibitors against Malarial Protease Plasmepsin
• Dipeptide-Type Inhibitors Targeting Plasmepsins from Plasmodium Falciparum
• Analysis of Side Reaction in the Amide Bond Formation with an α-Hydroxy-β-amino Acid as an Acyl Componemt
• Synthesis of Human C-Type Natriuretic Peptide 22 Using Chlorotrityl Resin and Tetrafluoroboric Acid Deprotection
• O-N Intramolecular Acyl and Acyloxy Migration Reaction in the Development of Water-Soluble Prodrugs of Taxoids
• Development of New Water-Soluble Prodrugs Based on Intramolecular Nucleophilic Reactions in Peptide Chemistry
• SYNTHESES AND STRUCTURE-ACTIVITY RELATIONSHIPS OF SMALL-SIZED ATRIAL NATRIURETIC PEPTIDE (ANP) DERIVATIVES
• Solid Phase Synthesis of a Mercaptoamide Peptide Using New Linkers
• Delivery of small interfering RNA with a synthetic collagen poly (Pro-Hyp-Gly) for gene silencing in vitro and in vivo
• Atelocollagen-mediated systemic administration of myostatin-targeting siRNA improves muscular atrophy in caveolin-3-deficient mice
• Click Peptide : Application to E22Δ-type Mutant of Amyloid β Peptide
• Click Peptide : In Situ Production of pyroGlu-Abeta from the O-Acyl Isopeptide
• Use of O-Acyl Isopeptides to Identify New Functions of Amyloid β Peptides
• Histidine-Related Dipeptides, Carnosine, Anserine and Homocarnosine, Possess the CNS Depressant Effects on Mice and their Action Mechanism
• Design and Preparation of the Tetrapeptides as Low Molecular Sized BACE1 Inhibitors
• Screening Methodology for Discovery of Inhibitory Peptides against Pathogenic Proteins using a Plug-plug Affinity Capillary Electrophoresis Technique
• Development of a Solid-supported Biotinylation Reagent for the Efficient Biotin Labeling to the SH group of Peptides and Small Molecules
• Optimization of Peptidomimetic Plasmepsin Inhibitor Containing Allophenylnorstatine Using Basic Substituent for Malaria Treatment
• Design of BACE1 Inhibitors Containing 5-Nitro-Isophthalamide
• Can the substrate of an enzyme turn into its inhibitor by vastly-reduced k_ value?
• Phenyl(cyclo)alkylamines : Second generation P_1' position analogs for pentapeptidic BACE1 inhibitors
• Tripeptidic BACE1 Inhibitors by Conformational Structure-based Design
• Structure Activity Relationship Study of SARS Coronavirus 3CL Protease Inhibitors with an Electrophilic Aryl Ketone Structure
• Synthesis and Biological Evaluation of Dipeptidic Antibiotics (+)-Negamycin and Its Derivatives for Development of Duchenne Muscular Dystrophy Chemotherapy
• Isotope Labeling-assisted Quantitative Evaluation of Refolding Conditions of a Recombinant Disulfide Protein
• Intact Cell-based SPR Analyses of Interactions between EGF and its Receptor
• Development of Chemical Probes towards the Elucidation of Binding Mechanism of Plinabulin, a Cyclicdipeptide Based Anti-microtubule Agent
• Novel BACE1 inhibitors containing P_1-P_1' non-natural amino acid-guanidinyl analogues
• Design, Synthesis and Evalution of Tripeptidomimetics with Arylketone as Inhibitors of SARS-CoV 3CL Protease
• Quantitative Analyses of Disulfide Bond Formation in Proteins Using ^O-Labeled Peptide Standards
• Novel Neutrophil-Activating Cryptides Hidden in Mitochondrial Cytochrome c : Identification and Structure-Activity Studies
• Design and SAR Study of Tripeptidic BACE1 Inhibitors
• Development of (+)-Negamycin Derivatives with Potent Readthrough Activity for Duchenne Muscular Dystrophy Chemotherapy
• Antihypertensive effects of CS-905, a novel dihydropyridine Ca++ channel blocker.

もっと見る 閉じる

スポンサーリンク