Synthesis and Platelet Aggregation-Inhibitory Activities of Novel 3-(2-Oxopropylidene)azetidin-2-one Derivatives. I
スポンサーリンク
概要
- 論文の詳細を見る
Treatment of (E)-3-(2-hydroxypropylidene)-4-methyl-1-phenylazetidin-2-one (11) with 10% Pd/C gave (E)-(12), (Z)-3-(2-oxopropylidene)-4-methyl-1-phenylazetidin-2-one (13), 3,4-cis-(14a) and 3,4-trans-3-(2-oxopropyl)-4-methyl-1-phenylazetidin-2-one (14b). Among them, 12 and 13 were found to show potent inhibitory activities against rabbit platelet-rich plasma aggregation induced by adenosine diphosphate or collagen. Ring-expanded homologous derivatives and an acyclic analogue-of 12 were also synthesized and tested for the biological activities. The azetidin-2-one skeleton bearing a 2-oxoalkylidene moiety at the 3 position was found to be essential for the platelet aggregation inhibitory activities of these compounds.
- 社団法人日本薬学会の論文
- 1990-02-25
著者
-
佐藤 正和
成均館大学校
-
佐藤 正和
大正製薬
-
川島 豊
Research Center, Taisho Pharmaceutical Co., Ltd.
-
佐藤 正和
Research Center, Taisho Pharmaceutical Co., Ltd.
-
畑田 祐一
Research Center, Taisho Pharmaceutical Co., Ltd.
-
中嶋 由茂元
Research Center, Taisho Pharmaceutical Co., Ltd.
-
中嶋 由茂元
Research Center Taisho Pharmaceutical Co. Ltd.
-
畑山 勝男
Research Center, Taisho Pharmaceutical Co., Ltd.,
-
五藤 准
Research Center Taisho Pharm. Co., Ltd.,
-
渋谷 皓
Tokyo College of Pharmacy
-
川島 豊
Research Center Taisho Pharmaceutical Co. Ltd.
-
川島 豊
大正製薬・総合研
-
畑田 祐一
Research Center Taisho Pharmaceutical Co. Ltd.
-
畑山 勝男
Research Center Taisho Pharmaceutical Co. Ltd.
-
佐藤 正基
School Of Pharmaceutical Sciences University Of Shizuoka(present Address):marusa Corporation
-
Sato M
Otsuka Pharmaceutical Co. Ltd. Tokushima Jpn
-
五藤 准
Research Center Taisho Pharm. Co. Ltd.
-
佐藤 真友美
Univ. Shizuoka Shizuoka Jpn
-
佐藤 正和
Research Center Taisho Pharmaceutical Co. Ltd.
-
Hatayama K
Research Center Taisho Pharmaceutical Co. Ltd.
-
畑田 祐一
Research Center, Taisho Pharmaceutical Co., Ltd.,
関連論文
- Furo[3,2-b]indole Derivatives. V. Synthesis and Structure-Activity Studies of 4-Substituted 2-(4-Methylpiperazinylcarbonyl)-6-trifluoromethylfuro[3,2-b]indole Derivatives with Analgesic and Antiinflammatory Activities(Medicinal Chemistry,Chemical)
- Stereoselective Permeation of New Fluorinated Quinolone Derivatives across LLC-PK_1 Cell Monolayers
- Uptake of Doxorubicin by Cultured Kidney Epithelial Cells LLC-PK_1
- ピロリドン誘導体によるPC12細胞の分化誘導
- 神経細胞分化誘導剤エポラクタエン類縁化合物の生物活性 : 有機化学・天然物化学
- RK-682誘導体のチロシンホスファターゼ阻害活性 : 有機化学・天然物化学
- Structure-Activity Relationship Study of TXA_2 Receptor Antagonists. 4-[2-(4-Substituted Phenylsulfonylamino)ethylthio]phenoxyacetic Acids and Related Compounds
- Synthesis and Evaluation of Novel Thiazolidine Derivatives as Thromboxane A_2 Receptor Antagonists
- Synthesis and Platelet Aggregation Inhibitory Activities of 3-(2-Oxopropylidene)azetidin-2-one Derivatives. II
- 微小試験片法による金属/セラミックス複合材料の破壊靭性評価
- 遊離アミノ酸組成からみた日韓両国国民の嗜好の相違(第1報) : キムチ及び漬物の遊離アミノ酸と嗜好
- Synthesis and Platelet Aggregation-Inhibitory Activities of Novel 3-(2-Oxopropylidene)azetidin-2-one Derivatives. I
- 炭素鋼表面き裂材の腐食疲労き裂進展挙動に関する破壊力学的研究
- 水素ガス環境下での低合金鋼のき裂進展挙動とAE放出特性の評価
- 自動車用排気浄化触媒の開発と実用化
- Furo[3,2-b]indole Derivatives. VI. Synthesis and Inhibitory Effect on Platelet Aggregation of Furo[3,2-b]indole Derivatives(Medical Chemistry,Chemical)
- Furo[3,2-b]indole Derivatives. III. : Structure-Activity Studies of 4,6-Disubstituted N-(3-Piperidinopropyl)furo[3,2-b]indole-2-carboxamide Derivatives for Analgesic and Antiinflammatory Activities
- AE周波数解析による銅ベリリウム・コバルト合金の破壊じん性ならびに微視破壊過程の評価
- Furo [3,2-b] indole Derivatives. II. Synthesis and Analgesic and Anti-inflammatory Activities of 4-Alkoxycarbonyl-2-morpholinocarbonylfuro [3,2-b] indole Derivatives
- 韓国の宮廷料理
- 海洋細菌に関する研究-2-海洋細菌の特異的無機塩要求性について〔英文〕
- 鎮痛・抗炎症活性を示すフロ-インド-ルカルボン酸アミドの定量的構造活性相関とドラッグデザイン (構造活性相関とドラッグデザイン)
- 製剤中のニトロプルシドナトリウム定量法に関する検討 : 直接吸光度法,スルフィド法,高速液体クロマトグラフ法についての検討
- 新規硬化療法剤の細胞障害作用
- Furo [3,2-b] indole Derivatives. I. Synthesis and Analgesic and Anti-inflammatory Activities of 4,6-Disubstituted-furo [3,2-b] indole-2-carboxamide Derivatives
- A Synthetic Application of Methylthioacetonitrile. I. A Synthesis of cis- and trans-β-Arylacrylonitriles, β, γ-Unsaturated Nitriles and Carbonyl Compounds
- Resistance of Hepatic Lysosomes, Mitochondria and Microsomes of Protoporphyrin-Administered Rats to Peroxidative Damage
- Antioxidative Effect of Protoporphyrin and Increase of Glutathione in Protoporphyrin-Administered Rat Liver
- プロトポルフィリン投与ラットにおけるポルフィリンの肝細胞内分布と抗脂質過酸化作用(生物学及び生化学)
- ANTIOXIDATIVE EFFECT OF SEVERAL PORPHYRINS ON LIPID PEROXIDATION IN RAT LIVER HOMOGENATES
- Effects of Sodium Metallochlorophyllins on the Activity and Components of the Microsomal Drug-Metabolizing Enzyme System in Rat Liver
- Effect of Sodium Copper Chlorophyllin on Lipid Peroxidation. IX. : On the Antioxidative Components in Commercial Preparations of Sodium Copper Chlorohyllin
- Effect of Sodium Copper Chlorophyllin on Lipid Peroxidation. VIII. Its Effect on Carbon Tetrachloride-Induced Liver Injury in Rats
- Effect of Sodium Copper Chlorophyllin on Lipid Peroxidation. VII. Effect of Its Administration on the Stability of Rat Liver Lysosomes
- Effect of Sodium Copper Chlorophyllin on Lipid Peroxidation. VI. Effect of Its Administration on Mitochondrial and Microsomal Lipid Peroxidation in Rat Liver
- Effect of Sodium Copper Chlorophyllin on Lipid Peroxidation. V. Effect on Peroxidative Damage of Rat Liver Lysosomes
- 市販銅クロロフィリンナトリウム中の1抗酸化成分について
- Structure-Activity Study of Antihypertensive 1,4-Dihydropyridine Derivatives Having Nitrooxyalkyl Moieties at the 3 and 5 Positions
- Synthesis and Antihypertensive Activities of New 1,4-Dihydropyridine Derivatives Containing Nitrooxyalkylester Moieties at the 3- and 5-Positions
- Synthesis and Antihypertensive Activities of New 1,4-Dihydropyridine Derivatives Containing a Nitrooxy Moiety at the 3-Ester Position
- J60 単環式フェノール系化合物のゴキブリ誘引摂食活性について(生理活性物質)
- Platelet Anti-aggregant Activity of 2,2-Dimethylthiazolidine Hydrochloride and 2-(4-Hydroxy-3-methoxyphenyl)thiazolidine
- The Transport of Ciprofloxacin in Cultured Kidney Epithelial Cells LLC-PK_1
- Studies on Topical Antiinflammatory Agents. IV., : 21-(Alkylthio)acetates and (Methylthio)methoxides of Corticosteroids
- Studies on Topical Antiinflammatory Agents. V. : 17-(Alkylthio)- and Methoxyalkanoates of Corticosteroids
- Studis on Topical Antiinflammatory Agents. III. : Synthesis of 17α-Acyloxy-9α-fluoro-11β-hydroxy-16β-methyl-1,4-pregnadiene-3,20-dione 21-Thio Dericatives and Related Compounds
- Studies on Topical Antiinflammatory Agents. II. Synthesis and Vasoconstrictive Activity of 21-Substituted Corticosteroids with Sulfur-Containing Moieties
- Facile Synthesis of 5α-Fluorocholestan-3-one from 4-Cholesten-3-one via Molecular Fluorine Addition and Reductive Defluorination
- Constituents of Chinese Crude Drug "Kushen"(the Root of Sophora flavescens AIT.). Isolation of Five New Flavonoids and Formononetin
- Studies on the Constituents of Guang-Dou-Gen (the Root of Sophora subprostrata CHUN et T.CHEN). (6). Isolation of Two New Flavanones
- Studies on the Constituents of Guang-Dou-Gen (the Root of Sophora subprostrata CHUN et T.CHEN). (5). Isolation of Two New Flavanones and Daidzein
- Bufadienolides. IX. Isolation and Structure of Resibufagin
- Studies on the Constituents of Sophora Species. V. Constituents of the Root of Sophora angustifolia SIEB. et ZUCC. (2)
- Studies on the Constituents of Sophora Species. II. Constituents of Sophora subprostrata CHUN et T. CHEN. (2). Isolation and Structure of New Flavonoids, Sophoradochromene and Sophoranochromene
- Studies on the Constituents of Sophora Species. I. Constituents of Sophora subprostrata CHUN et T. CHEN. (1). Isolation and Structure of New Flavonoids, Sophoradin and Sophoranone
- Structures of New Flavonoids, Sophoradochromene and Sophoranochromene, from Sophora subprostrata
- Structures of New Flavonoids, Sophoradin and Sophoranone, from Sophora subprostrata
- Studies on Selectivity of O-Methylation of Erythromycin Derivatives Based on Molecular Mechanics and Molecular Orbital Methods
- Structure-Activity Relationship Study of 6-O-Methylerythromycin 9-O-Substituted Oxime Derivatives
- 24 エリスロマイシン誘導体のO-メチル化における位置選択性について(口頭発表の部)
- Structure-Activity Studies of 3-Benzoylpropionic Acid Derivatives Suppressing Adjuvant Arthritis
- Effect of Protoporphyrin on Peroxidative Damage of Rat Liver Lysosomes
- Antioxidative Effect of Protoporphyrin on Lipid Peroxidation in Rat Liver Subcellular Fractions
- m-ジクロロベンゼン及びその含硫代謝物のマウス肝薬物代謝酵素系に及ぼす影響
- ラット肝可溶性画分存在下におけるミクロゾームの脂質過酸化におよぼすNADPHの影響
- ALUMINUM-MEDIATED ONE-POT CONVERSION OF α-AMINO ACID ESTERS TO THREO 2-AMINO ALCOHOLS WITH HIGH DIASTEREOSELECTIVITY
- A Highly Diastereoselective Synthesis of cis-4a-Aryloctahydro-cyclopenta[c]pyridine Derivatives through Tandem Radical Cyclization of α-Amino Radical-Polyene Species
- A Synthesis of Simple 4,4-Disubstituted Tetrahydroisoquinolines by Cyclization of α, α-Disubstituted Phenylacetamides
- Pharmacokinetics of Granisetron in Adults and Children with Malignant Diseases
- A Rapid Assay of Granisetron in Biological Fluids from Cancer Patients.
- A Rapid Assay of Granisetron in Biological Fluids from Cancer Patients
- Anti-ulcer Effect of Isoprenyl Flavonoids. II. Synthesis and Anti-ulcer Activity of New Chalcones related to Sophoradin
- Synthesis and Antiinflammatory Activity of Alkenylphenylpropionic Acids
- Synthesis and Pharmacological Evaluation of 1,2,3,4-Tetrahydro-β-carboline Derivatives
- Mild and Facile Cleavage of 2-Cyanoethyl Ester Using Sodium Sulfide or Tetrabutylammonium Fluoride. Synthesis of 1,4-Dihydropyridine Monocarboxylic Acids and Unsymmetrical 1,4-Dihydropyridine Dicarboxylates
- Protecting Group for Carboxyl Function : Mild and Facile Cleavage of 2-Cyanoethyl Ester under Non-hydrolytic Conditions
- Anti-ulcer Effect of Isoprenyl Flavonoids. III. Synthesis and Anti-ulcer Activity of Metabolites of 2'-Carboxymethoxy-4,4'-bis (3-methyl-2-butenyloxy) chalcone
- 遊離アミノ酸組成からみた日韓両国国民の嗜好の相違(第1報) : キムチ及び漬物の遊離アミノ酸と嗜好
- 酸窒化処理の自動車部品と金型への適用
- Sex Differences in Constitutive Level of Renal Lauric Acid Hydroxylase Activities and CYP4A-Related Proteins in Mice
- Sex and Strain Differences in Constitutive Expression of Fatty Acid ω-Hydroxylase (CYP4A-Related Proteins) in Mice
- Effects of Gonadectomy and Sex Hormones on the Induction of Hepatic CYP4A by Clofibrate in Rats
- Dehydrotrametenolic Acid Induces Preadipocyte Differentiation and Sensitizes Animal Models of Noninsulin-Dependent Diabetes Mellitus to Insulin
- In Vivo Drug Release and Antitumor Characteristics of Water-Soluble Conjugates of Mitomycin C with Glycol-Chitosan and N-Succinyl-Chitosan
- Studies on the Constituents of Sophora Species. VI. Constituents of the Root of Sophora subprostrata CHUN et T. CHEN. (4)
- Highly Diastereoselective Synthesis of (3R, 4R)- and (3R, 4S)-β, γ-Diamino Acids from D-Phenylalanine
- Diastereoconversion of 1-Alkynyl-2-aminoalkanols through Oxazoline-2-ones with S_N2 Type Inversion of the Hydroxy Group
- 自動車産業と新素材開発--テクノアメニティを求めて
- メタノ-ルの燃料化
- The Stevens Rearrangement of Quarternary Isoquinolinium Salts
- Formation of Dibenzo [b, f] azecines by the Reaction of 1-Halogenophenethyl-1H-2-benzazepines with Dimsylsodium
- A Synthesis of Dibenz [b, f] azecines from 1-Halogenobenzyl-1H-2-benzazepines
- N-Demethylation of Dibenz [b, f] azonines with Mercuric Acetate
- Syntheses of Dibenzo [b, g] azecines and Dibenzo [b, f] azonines
- Synthesis of the Ochotensine Type 1-Spiroisoquinoline. Dimsylsodiuminduced Rearrangement of N-Methyltetrahydroprotoberberinium Salts
- Syntheses of 13a-Substituted Dibenzo [a, f] quinolizines
- Novel Syntheses of 5,6,12,12a-Tetrahydro-12a-methyldibenzo-[b, g] indolizine Systems
- Intra- and Intermolecular Nucleophilic Cleavage of the Amide Bond of β-Lactams
- Syntheses of Dibenzo [b, f] azonines and Dibenzo [b, g] azecines through Ring Expansion of 1-Substituted Isoquinolines
- The C-N Fission of Dibenzo [b, g] indolizinium Salts with Dimsylsodium