Synthesis of Antimicrobial Agents. III. Synthesis and Antimicrobial Activities of Thiazolo [5,4-b] naphthyridine Derivatives
スポンサーリンク
概要
- 論文の詳細を見る
In order to search for new antimicrobial agents, a number of 2-substituted 8-ethyl-5,8-dihydro-5-oxothiazolo [5,4-b] naphthyridine-6-carboxylic acid and their related compounds which consist of a new ring system were prepared. Reactions of the 6-amino-1-ethyl-7-mercapto-1,4-dihydro-4-oxonaphthyridine-3-carboxylic acid (2) with acid, acid anhydride, acid chloride and ethylxanthate afforded several thiazolo [5,4-b] naphthyridine derivatives. Refluxing ethyl 7-chloro-1-ethyl-6-nitro-1,4-dihydro-4-oxonaphthyridine-3-carboxylate (16) with KSCN in acetic acid gave directly the thiazole cyclization product 19. Reaction of 8-ethyl-2-methylthio-5,8-dihydro-5-oxothiazolo [5,4-b] naphthyridine-6-carboxylic acid (11) with dimethyl sulfate gave various products (13b, 25 and 26) depending upon its reaction conditions. Some compounds obtained in this work exhibited high activities against gram-negative and gram-positive bacteria in vitro.
- 公益社団法人日本薬学会の論文
- 1979-02-25
著者
-
鈴木 範夫
Research Institute, Daiichi Seiyaku Co., Ltd.
-
鈴木 範夫
Research Institute Daiichi Seiyaku Co. Ltd.
-
堂森 廉三
Research Institute Daiichi Seiyaku Co. Ltd.
関連論文
- Synthesis of Antimicrobial Agents. VII. Synthesis and Antibacterial Activities of Furo [2,3-g] quinoline Derivatives
- Synthesis of Antimicrobial Agents. VI. Studies on the Synthesis of Furo [3,2-b] [1,8] naphthyridine Derivatives
- 含フッ素ピリミジン系スルファニルアミド誘導体の合成と抗菌性
- Studies on Pyrimidinylpyrazoles. II. Ring Closures of N^2-Pyrimidinyl-3-oxobutyrohydrazides
- The Metabolic Fate of 1-(4-Methoxy-6-methyl-2-pyrimidinyl)-3-methyl-5-methoxypyrazole (Mepirizole, DA-398) in Rats and Rabbits
- 化学療法薬の合成(第2報)1,8-Naphthyridine誘導体の合成と抗トリコモナス活性
- Synthesis of Antimicrobial Agents. IV. Synthesis and Antimicrobial Activities of Imidazo [4,5-b] [1,8] naphthyridine Derivatives
- Synthesis of Antimicrobial Agents. III. Synthesis and Antimicrobial Activities of Thiazolo [5,4-b] naphthyridine Derivatives
- Synthesis of Antimicrobial Agents. I. Synthesis and Antimicrobial Activities of Thiazoloquinoline Derivatives
- ナリジクス酸関連化合物研究の現況 (新しい医薬品の開発)
- Synthetic Chemotherapeutic Agents. IV. Synthesis of 3-Substituted Thiazolo [5,4-f] quinoline Derivatives. (2)
- Synthetic Chemotherapeutic Agents. III. Synthesis of 3-Substituted Thiazolo [5,4-f] quinoline Derivatives. (1)
- Synthetic Chemotherapeutic Agents. II. Synthesis of 2-Substituted Thiazolo [5,4-f] quinoline Derivatives. (2)
- Synthetic Chemotherapeutic Agents. I. Synthesis of 2-Substituted Thiazolo [5,4-f] quinoline Derivatives. (1)
- Syntheses of the Urinary Metabolites of 1-(4-Methoxy-6-methyl-2-pyrimidinyl)-3-methyl-5-methoxypyrazole (Mepirizole, DA-398)
- Synthesis of 1-Substituted 1,4-Dihydro-7-[2-(5-nitro-2-furyl) vinyl]-4-oxo-1,8-naphthyridine Derivatives. II
- Synthesis of 1-Substituted 1,4-Dihydro-7-[2-(5-nitro-2-furyl) vinyl]-4-oxo-1,8-naphthyridine Derivatives. I
- Rearrangement of Sulfonamide Derivatives. V. Syntheses of Methyl α-Phenyl-2- and 4-piperidineacetate.
- スルフォンアミド誘導体の転位反応(第4報)ピリジン及びキノリン1-オキシドのスルフォンアミド誘導体の転位反応
- スルフォンアミド誘導体の転位反応(第3報)反応機構に就いての考察
- Synthesis of Antimicrobial Agents. V. Synthesis and Antimicrobial Activities of Some Heterocyclic Condensed 1,8-Naphthyridine Derivatives