Synthesis and Anti-influenza Evaluation of Polyvalent Sialidase Inhibitors Bearing 4-Guanidino-Neu5Ac2en Derivatives
スポンサーリンク
概要
- 論文の詳細を見る
Polyvalent sialidase inhibitors bearing 4-guanidino-Neu5Ac2en derivatives on a poly-L-glutamine backbone are described. Aiming for a longer retention time of 4-guanidino-Neu5Ac2en (zanamivir) in bronchi and lungs, we focused on supermolecules bearing 4-guanidino-Neu5Ac2en derivatives bound at their C-7 position through noncleavable alkyl ether linkages. We first found that alkylation of the 7-hydroxyl group of sialic acid derivative 8 proceeded smoothly, and produced 7-O-alkyl-4-guanidino-Neu5Ac2en derivatives 13, which exhibited equipotenl inhibitory activity against not only influenza A virus sialidase but also influenza A virus in the cell culture. Next. we synthesized poly-L-glutamine bearing 7-O-alkyl-4-guanidino-Neu5Ac2en derivatives linked by amide bonds. 26, which showed enhanced antiviral activity against influenza A virus and more potent efficacy in vivo relative to a monomeric sialidase inhibitor.
- 公益社団法人日本薬学会の論文
- 2003-12-01
著者
-
Yamashita Makoto
Biological Research Laboratories, Daiichi Sankyo Co., Ltd.
-
Honda T
Medicinal Chemistry Research Laboratories Sankyo Co. Ltd.
-
Arai Masami
Medicinal Chemistry Research Laboratories Sankyo Co. Ltd.
-
Yamashita M
Biological Research Laboratories Sankyo Co. Ltd.
-
MASUDA Takeshi
Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd.
-
YOSHIDA Shuku
Biological Research Laboratories, Sankyo Co., Ltd.
-
KANEKO Satoru
Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd.
-
HONDA Takeshi
Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd.
-
吉田 茂男
The Institute Of Physical And Chemical Research
-
Honda Takeshi
Medicinal Chemistry Research Laboratories 1 Daiichi Sankyo Co. Ltd.
-
Yoshida S
Biological Research Laboratories Sankyo Co. Ltd.
-
Kaneko S
Medicinal Chemistry Research Laboratories Sankyo Co. Ltd.
-
Masuda Takeshi
Daiichi Sankyo Co. Ltd. Tokyo Jpn
-
Yamashita Makoto
Biological Research Laboratories Sankyo Co. Ltd.
-
Masuda Takeshi
Medicinal Chemistry Research Laboratories Ii Daiichi Sankyo Co. Ltd.
-
Yamashita Makoto
Biological Research Laboratories Daiichi Sankyo Co. Ltd.
関連論文
- RS-1748, a Novel CC Chemokine Receptor 4 Antagonist, Inhibits Ovalbumin-Induced Airway Inflammation in Guinea Pigs
- スズメノカタビラの s-トリアジン除草剤抵抗性の分子機構および異なる光条件下における光合成機能
- Screening of Inhibitor of Eukaryotic DNA Polymerases Produced by Microorganisms
- Diacylated 8-C-Glucosylcyanidin 3-Glucoside from the Flowers of Tricyrtis formosana
- One-Pot Preparation of Chiral β-Amino Esters by Rhodium-Catalyzed Three-Components Coupling Reaction
- Selective Synthesis of β-Amino Esters and β-Lactams by Rhodium-catalyzed Reformatsky-Type Reaction
- Galactosyldiacylglycerol, a Mammalian DNA Polymerase α-Specific Inhibitor from a Sea Alga, Petalonia bingbamiae
- The Cyanogenic Glucoside, Prunasin (D-Mandelonitrile-β-D-Glucoside), Is a Novel Inhibitor of DNA Polymerase β
- Action of a New Mammalian DNA Polymerase Inhibitor, Sulfoquinovosyldiacylglycerol
- Sulfoquinovosyldiacylglycerol, KM043,a New Potent Inhibitor of Eukaryotic DNA Polymerases and HIV-Reverse Transcriptase Type 1 from a Marine Red Alga, Gigartina tenella
- Synthesis and Anti-influenza Evaluation of Polyvalent Sialidase Inhibitors Bearing 4-Guanidino-Neu5Ac2en Derivatives
- Four Euglobals from Eucalyptus blakelyi
- Inhibitors of Skin-Tumor Promotion. VIII. : Inhibitory Effects of Euglobals and Their Related Compounds on Epstein-Barr Virus Activation. (1)
- Separation of Stereoisomers of Some Terpene Derivatives by Capillary Gas Chromatography-Mass Spectrometry and High-Performance Liquid Chromatography Using β-Cyclodextrin Derivative Columns
- Analyses of Anandamide and Endocannabinoid-like Compounds Using Collision-induced Dissociation in Fast Atom Bombardment Ionization-Mass Spectrometry and Gas Chromatography/Chemical Ionization-Mass Spectrometry
- Non-glutamate Type Pyrrolo[2,3-d]pyrimidine Antifolates. III. Synthesis and Biological Properties of N^ω-Masked Ornithine Analogs
- Non-glutamate Type Pyrrolo[2,3-d]pyrimidine Antifolates. II. Synthesis and Antitumor Activity of N^5-Substituted Glutamine Analogs
- Synthesis of 4-Guanidino-7-Modified-Neu5Ac2en Derivatives and Their Biological Activities as Influenza Sialidase Inhibitors
- Studies on High-energy Collision-induced Dissociation of Endogenous Cannabinoids : 2-Arachidonoylglycerol and N-Arachidonoylethanolamide in FAB-Mass Spectrometry
- Allixin Accumulation with Long-term Storage of Garlic
- High and continuous exposure of laninamivir, an anti-influenza drug, may work suppressively to generate low-susceptibility mutants in animals
- Anti-Pseudomonas aeruginosa Compound, 1,2,3,4-Tetrahydro-1,3,5-triazine Derivative, Exerts Its Action by Primarily Targeting MreB