Novel Phenoxyalkylamine Derivatives. VII. Synthesis and Pharmacological Activities of 2-Alkoxy-5-[(Phenoxyalkylamino)alkyl]benzenesulfonamide Derivatives

スポンサーリンク

概要

• 論文の詳細を見る

• To find a novel α-blocker with high α-blocking selectivity against dopamine D_2-receptor affinity, we performed structural modification of the alkylene chains and the substituents on two benzene rings of 2-alkoxy-5-[(phenoxyalkylamino)alkyl]benzenesulfonamide derivatives. The modification of the alkylene chain between the amino moiety in the center of the molecule and the benzene ring (ring A) was found to be the most significant. 5-[2-[[2-(5-Fluoro-2-methoxyphenoxy)ethyl]amino]propyl]-2-methoxybenzenesulfonamide (II-4), which possesses 1-methylethyl as the alkylene chain, exhibited high α-blocking selectivity as well as potent α-blocking activity.

• 社団法人日本薬学会の論文
• 1992-06-25

著者

• 加藤 日出男

  北陸製薬株式会社

• 森川 宏二

  北陸製薬株式会社

• 桜井 俊一郎

  北陸製薬株式会社中央研究所研究開発本部

• 安田 信吾

  北陸製薬株式会社中央研究所研究開発本部

• 越中 栄一

  Research and Development Division, Hokuriku Seiyaku Co., Ltd.,

• 伊藤 安夫

  Research and Development Division, Hokuriku Seiyaku Co., Ltd.,

• 加藤 日出男

  Central Research Laboratories, Hokuriku Seiyaku Co., Ltd.,

• 伊藤 安夫

  Central Research Laboratories, Hokuriku Seiyaku Co., Ltd.,

• 桜井 俊一郎

  Central Research Laboratory, Hokuriku Seiyaku Co., Ltd.,

• 見谷 一也

  Central Research Laboratory, Hokuriku Seiyaku Co., Ltd.,

• 橋本 繁輝

  Central Research Laboratory, Hokuriku Seiyaku Co., Ltd.,

• 森川 宏二

  Central Research Laboratory, Hokuriku Seiyaku Co., Ltd.,

• 安田 信吾

  Central Research Laboratory, Hokuriku Seiyaku Co., Ltd.,

• 越中 栄一

  Central Research Laboratory, Hokuriku Seiyaku Co., Ltd.,

• 越中 栄一

  Research And Development Division Hokuriku Seiyaku Co. Ltd.

• 伊藤 安夫

  Research And Development Division Hokuriku Seiyaku Co. Ltd.

• 橋本 繁輝

  Central Research Laboratory Hokuriku Seiyaku Co. Ltd.

• 見谷 一也

  Central Research Laboratory Hokuriku Seiyaku Co. Ltd.

• 加藤 日出男

  北陸製薬株式会社中央研究所

関連論文

• 気管支喘息治療薬ツロブテロールの経皮吸収型製剤の開発
• 232 新規TXA_2/LTD_4デュアル拮抗薬RS-601の抗喘息作用
• Benzenesulfonamide誘導体の合成とThromboxane A_2及びLeukotriene D_4に対するDual拮抗作用
• Amphoteric Drugs. II. Synthesis and Antiallergic Activity of [4-(5H-Dibenzo[a, d]cycloheptan-5-ylidene)piperidino]alkanoic Acid Derivatives and Related Compounds
• Amphoteric Drugs. I. Synthesis and Antiallergic Activity of [4-(Diphenylmethoxy)piperidino]-, [4-(Diphenylmethyl)piperazinyl]-and [4-(Diphenylmethylene)piperidino]alkanoic Acid Derivatives
• Transport Mechanism of an H_1-Antagonist at the Blood-Brain Barrier : Transport Mechanism of Mepyramine Using the Carotid Injection Technique
• 医薬品の両性イオン化(第3報)1,2,3,4,10,14b-Hexahydrodibenzo-[c, f]pyrazino[1,2-α]azepine及び2,3,4,9-Tetrahydro-1H-dibenzo[3,4 : 6,7]cyclohepta[1,2-c]pyridineのN-Alkylcarboxylic Acid誘導体の合成とその薬理作用
• Study on Zwitter-Ionization of Drugs. II. Synthesis and Pharmacological Activity of Some N-[3-(5H-Dibenzo[a, d]cyclohepten-5-ylidene)propyl]-N-methylamino- and N-[3-(6H-Dibenz[b, e]oxepin-11-ylidene)propyl]-N-methylamino-alkanoic Acid Derivatives and Rela
• INTER-INDIVIDUAL DIFFERENCES OF (+)-4-[4-(4-METHYLPHENYL)PHENYLMETHOXY-1-PIPERIDINYL]BUTYRIC ACID ((+)-MPPB) DISPOSITION IN RATS
• 医薬品の両性イオン化(第1報)4-(2-Chlorodibenz[b, f][1,4]oxazepin-11-yl)piaerazine, 4-(2-Chlorodibenzo[b, f][1,4]thiazepin-11-yl)-piperazine及び4-(11H-Dibenz[b, e]azepin-6-yl)piperazineのN-アルキルカルボン酸誘導体の合成とその薬理作用
• Novel Phenoxyalkylamine Derivatives. VII. Synthesis and Pharmacological Activities of 2-Alkoxy-5-[(Phenoxyalkylamino)alkyl]benzenesulfonamide Derivatives
• Synthesis, Gastrointestinal Prokinetic Activity and Structure-Activity Relationships of Novel N-[[2-(Dialkylamino)ethoxy)benzyl]benzamide Derivatives
• Quinolone系抗菌剤の研究(第3報)5-Amino-7-(2-aminoalkoxy)-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic Acid及びその関連化合物の合成と抗菌活性
• Ouinolone系抗菌剤の研究(第2報)7-Aminoalkoxy-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic Acid及びその関連化合物の合成と抗菌活性
• 新規なPhenoxyalkylamine誘導体(第6報)α-[(Phenoxyethylamino)propyl]-α-phenylacetonitrile誘導体の合成とα-遮断作用
• Studies on Antiallergic Agents. II. : Quantitative Structure-Activity Relationships of Novel 6-Substituted N-(1H-Tetrazol-5-yl)-2-pyrazinecarboxamides
• Quinolone系抗菌剤の研究(第1報)7-(2-Aminoethoxy)-, 7-(2-Aminoethylthio)-及び7-(2-Aminoethylamino)-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic Acid及びそれらの誘導体の合成と抗菌活性
• Studies on Antiallergic Agents. I. : Synthesis and Antiallergic Activity of Novel Pyrazine Derivatives
• Novel Phenoxyalkylamine Derivatives. V. : Synthesis, α-Blocking Activity and Quantitative Structure-Activity Analysis of α-[(Phenoxyethylamino)propyl]-α-phenylacetonitrile Derivatives
• Novel Phenoxyalkylamine Derivatives. IV. : Synthesis, Ca^-Antagonistic Activity and Quantitative Structure-Activity Analysis of α-Isopropyl-α-[3[3-(3-methoxyphenoxy)propylamino]propyl]-α-phenylacetonitrile Derivatives
• Synthesis and Histamine H_2-Antagonist Activity of 4-Quinazolinone Derivatives
• Novel Phenoxyalkylamine Derivatives. III. : Quantitative Structure-Activity Relationships of Ca^-Antagonistic α-Alkyla-α-[(phenoxypropylamino)propyl]-3,4,5-trimethoxy-benzeneacetonitrile Derivatives
• Novel Phenoxyalkylamine Derivatives. II. : Synthesis and Ca^-Antagonistic Activities of α-Alkyl-α-[(phenoxypropylamino)propyl]-benzeneacetonitrile Derivatives
• Novel Phenoxyalkylamine Derivatives. I. : Synthesis and Pharmacological Activities of α-Isopropyl-α-[(phenoxyalkylamino)alkyl]-benzeneacetonitrile Derivatives
• (2-Pyrimidinylamino)phenylacetic Acid誘導体の合成と抗炎症作用
• Dexamethasone valerate (DV-17) と他の副腎皮質ステロイド外用剤のラット比較毒性試験
• Dexamethasone valerate (DV-17)と他の副腎皮質ステロイド外用剤のウサギにおける刺激性試験 : 皮膚および眼粘膜一次刺激性試験ならびに皮膚累積刺激性試験
• Study on Zwitter-Ionization of Drugs. II. Synthesis and Pharmacological Activity of Some N-[3-(5H-Dibenzo[a, d]cyclohepten-5-ylidene)propyl]-N-methylamino- and N-[3-(6H-Dibenz[b, e]oxepin-11-ylidene)propyl]-N-methylamino-alkanoic Acid Derivatives and Rela
• Study on Zwitter-Ionization of Drugs. II. Synthesis and Pharmacological Activity of Some N-[3-(5H-Dibenzo[a, d]cyclohepten-5-ylidene)propyl]-N-methylamino- and N-[3-(6H-Dibenz[b, e]oxepin-11-ylidene)propyl]-N-methylamino-alkanoic Acid Derivatives and Rela
• Study on Zwitter-Ionization of Drugs. II. Synthesis and Pharmacological Activity of Some N-[3-(5H-Dibenzo[a, d]cyclohepten-5-ylidene)propyl]-N-methylamino- and N-[3-(6H-Dibenz[b, e]oxepin-11-ylidene)propyl]-N-methylamino-alkanoic Acid Derivatives and Rela
• Study on Zwitter-Ionization of Drugs. II. Synthesis and Pharmacological Activity of Some N-[3-(5H-Dibenzo[a, d]cyclohepten-5-ylidene)propyl]-N-methylamino- and N-[3-(6H-Dibenz[b, e]oxepin-11-ylidene)propyl]-N-methylamino-alkanoic Acid Derivatives and Rela
• Study on Zwitter-Ionization of Drugs. II. Synthesis and Pharmacological Activity of Some N-[3-(5H-Dibenzo[a, d]cyclohepten-5-ylidene)propyl]-N-methylamino- and N-[3-(6H-Dibenz[b, e]oxepin-11-ylidene)propyl]-N-methylamino-alkanoic Acid Derivatives and Rela
• Study on Zwitter-Ionization of Drugs. II. Synthesis and Pharmacological Activity of Some N-[3-(5H-Dibenzo[a, d]cyclohepten-5-ylidene)propyl]-N-methylamino- and N-[3-(6H-Dibenz[b, e]oxepin-11-ylidene)propyl]-N-methylamino-alkanoic Acid Derivatives and Rela
• Study on Zwitter-Ionization of Drugs. II. Synthesis and Pharmacological Activity of Some N-[3-(5H-Dibenzo[a, d]cyclohepten-5-ylidene)propyl]-N-methylamino- and N-[3-(6H-Dibenz[b, e]oxepin-11-ylidene)propyl]-N-methylamino-alkanoic Acid Derivatives and Rela
• Study on Zwitter-Ionization of Drugs. II. Synthesis and Pharmacological Activity of Some N-[3-(5H-Dibenzo[a, d]cyclohepten-5-ylidene)propyl]-N-methylamino- and N-[3-(6H-Dibenz[b, e]oxepin-11-ylidene)propyl]-N-methylamino-alkanoic Acid Derivatives and Rela
• Crystal Structures of Polymorphs of α-[(tert-Butylamino) methyl]-2-chloro-4-hydroxybenzyl Alcohol Hydrochloride (HOKU-81)
• 鎮痙剤の研究(第7報)N-Alkyl Diarylmethylenequinolizidinium Bromides, N-Alkyl Diarylmethyleneindolizidinium Bromidesおよび関連化合物の構造活性相関
• 鎮痙薬の薬理学的研究(第1報)Diarylmethylene-5-methyl-transquinolizidinium Bromide類の鎮痙作用への選択性
• Studies on Antispasmodics. VI. Synthesis of N-Alkyl 6- and 7-Diarylmethyleneindolizidinium Bromides
• Studies on Antispasmodics. V. Synthesis and Anticholinergic Activity of N-Alkyl 1- and 2-Diarylmethylene-indolizidinium Bromides
• 鎮痙剤の研究(第4報)Diarylhydroxymethylquinolizidine Methohalidesの合成と抗アセチルコリン作用
• 鎮痙剤の研究(第3報)2位置換Quinolizidine類の簡便な新合成法とそれらの立体構造について
• 鎮痙剤の研究(第2報)3位置換Quinolizidine類の簡便な新合成法とそれらの立体構造について
• Studies on Antispasmodics. I. Synthesis and Anticholinergic Activity of 1-, 2-, and 3-Diarylmethylenequinolizidine Quaternary Ammonium Salts
• o-Chloro-α-(tert-butylaminomethyl)benzylalcohol Hydrochloride(C-78)および関連化合物の合成と気管支拡張作用
• Studies on 1-Azabicyclo Compounds. XXVI. Synthesis of Ten-membered Ring Amines from 9a-Cyanomethyl-, 9a-Ethoxycarbonylmethyl-, and 1-Ethoxycarbonyl-octahydroquinolizine
• Chemical Transformation of Protoberberines. VIII. A Novel Synthesis of (±)-Fumaricine and a Formal Synthesis of (±)-Alpinigenine
• Studies on the Relationship between Physico-chemical Properties and Crystalline Forms of Tulobuterol Hydrochloride. II. Crystal Structure Analyses of the Four Crystalline Forms of Tulobuterol Hydrochloride
• 2-Methyl-3-pyrrolidinopropiophenone誘導体の中枢性筋弛緩作用
• Tulobuterolの生体内運命(第5報)ラット, イヌ, モルモットおよびウサギにおける代謝および排泄に関する種差
• ツロブテロールの生体内運命(第4報)ラット日齢と生体内動態について
• 塩酸ツロブテールの性状と結晶形との相関に関する研究(第3報) : 塩酸ツロブテール多形の吸湿特性
• 塩酸ツロブテロールの性状と結晶形との相関に関する研究(第3報)塩酸ツロブテロール多形の吸湿特性
• Studies on the Relationship between Physico-chemical Properties and Crystalline Forms of Tulobuterol Hydrochloride. I. Polymorphism of Tulobuterol Hydrochloride
• 胃粘膜微小循環に及ぼす3-(Di-2-thienylmethylene)-5-methyl-trans-quinolizidinium Bromide(HSR-902)の影響
• 54 8,14-Cycloberbineを経由するProtoberberineアルカロイドからSpirobenzylisoquinoline及びBenzindenoazepineアルカロイドの合成
• TRANSFORMATION OF PROTOBERBERINES INTO SPIROBENZYLISOQUINOLINES. STEREOSELECTIVE CONVERSION OF COPTISINE INTO (±)-OCHROBIRINE
• EFFICIENT CONVERSION OF PROTOBERBERINES INTO BENZINDENOAZEPINES. A FORMAL SYNTHESIS OF (±)-cis-ALPINIGENINE AND (±)-cis-ALPININE
• Polymorphism of α-[(tert-Butylamino) methyl]-2-chloro-4-hydroxybenzyl Alcohol Hydrochloride (HOKU-81)
• 1-Azabicyclo化合物の研究(第21報)1,2,3,10,11,11a-Hexahydro-5H-pyrrolo-[2,1-c][1,4]benzodiazepin-11-oneおよび5,6,6a, 7,8,9,10,12-Octahydropyrido[2,1-c][1,4]benzodiazepin-6-oneから中環状AminolactamおよびSpiroaminolactam体の合成
• Studies on 1-Azabicyclo Compounds. XVI. Synthesis of 1'-Methylindan-2-spiro-2'-piperazine and Related Compounds
• Studies on 1-Azabicyclo Compounds. XV. Oxidation of 1,3,4,6,11,11a-Hexahydro-2H-pyrazino [1,2-b] isoquinolin-1-one Derivatives with Mercuric Acetate, and Their Conversion into 1,2,3,4,5,6,7,8-Octahydro-2-methyl-2,5-benzodiazecine and Related Compounds
• 1-Azabicyclo化合物の研究その5 : 4-Oxoquinolizidineの水素化リチウムアルミニウム還元およびQuinolizidineの酢酸第二水銀酸化により得られた二量体の化学構造
• Tiquizium bromide (HSR-902) の急性胃粘膜損傷に対するCytoprotective作用とその機序
• Tiquizium bromide(HSR-902)の抗潰瘍薬としての評価
• Diazabicycloalkanesの研究(第2報)4-[β-(10-Phenothiazinyl)-ethyl]-1,4-diazabicyclo[4,4,0]-decaneおよび類似化合物の抗ヒスタミン作用ならびに向精神作用
• 臭化チキジウム
• 鎮痙薬の薬理学的研究(第5報) : 3-(Di-2-Thienylmethylene)-5-Methyl-trans-Quinolizidinium Bromide (HSR-902) の骨盤神経終末と膀胱壁筋との神経伝達に及ぼす作用
• 鎮痙薬の薬理学的研究(第3報)　3-(Di-2-Thienylmethylene)-5-Methyl-trans-QuinolizidiniumBromide(HSR-902)の鎮痙作用とその臓器特異性
• 3-(5-Nitro-2-furyl)-benzo-1,2,4-triazine誘導体の合成ならびに抗細菌作用について
• (±)-4-Ethyl-2-methyl-3-(1-pyrrolidinyl) propiophenone hydrochloride(HY-770)の膀胱機能に及ぼす作用
• 新しい頻尿治療薬3-Methy1-4-oxo-2-phenyl-N-[2-(1-piperidinyl)ethyl]-4H-1-benzopyran-8-carboxamide hydrochloride monohydrate(FL155)の麻酔下ラットの律動的膀胱収縮に対する作用
• 1-Azabicyclo化合物の研究(第20報)Hexahydroisoquino[3,2-c][1,4]benzodiazepineおよび関連化合物の合成ならびにHexahydroisoquino[3,2-c]-[1,4]benzodiazepin-13-one から6-Methyl-hexahydro-5H-dibenzo[b, g][1,5]diazacycloundecineの生成
• 1-Azabicyclo化合物の研究(第25報)Octahydropyrrolo[1,2-α]pyrazin-1-oneから9員環状Aminolactamおよび関連化合物の合成

もっと見る 閉じる

スポンサーリンク