3-Trifluoromethylcephalosporins. II. Synthesis and in Vitro Antibacterial Activities of 3-Trifluoromethylcephalosporin Derivatives
スポンサーリンク
概要
- 論文の詳細を見る
Various acylamido derivatives of 3-trifluoromethyl-3-cephem-4-carboxylic acid were synthesized and tested for in vitro antibacterial activities. The 3-trifluoromethylcephalosporin derivatives synthesized herein are 7α- and 7β-acylamido-3-cephem-, 7α- methoxy-7β-acylamido-3-cephem- and 7β-acylamido-2-cephem-4-carboxylic acids. Among these compounds, the R-mandelamido derivative (IIIb) showed the highest antibacterial activity against gram-negative bacteria at pH 7.0. The minimum inhibitory concentration values of the 2-thienylacetamido- and phenylglycylamido derivatives are compared with those of the 3-methyl- and 3-chloro analogs, and structure-activity relationships are discussed.
- 社団法人日本薬学会の論文
- 1980-01-25
著者
-
宮寺 哲男
Central Research Laboratories, Sankyo Co., Ltd.
-
渡辺 泰一郎
Chemical Research Laboratories Sankyo Co. Ltd.
-
西村 卓三
Central Research Laboratories Sankyo Co., Ltd.
-
渡辺 泰一郎
Central Research Laboratories, Sankyo Co., Ltd.
-
宮寺 哲男
Chemical Research Laboratories, Sankyo Co., Ltd.
-
川野 洋一
Central Research Laboratories, Sankyo Co., Ltd.
-
酒井 純一
Central Research Laboratories, Sankyo Co., Ltd.
-
渡辺 英俊
Central Research Laboratories, Sankyo Co., Ltd.
-
長野 光男
Central Research Laboratories, Sankyo Co., Ltd.
-
渡辺 英俊
Chemical Research Laboratories Sankyo Co. Ltd.
-
川野 洋一
Central Research Laboratories Sankyo Co. Ltd.
-
宮寺 哲男
Chemical Research Laboratories Sankyo Co. Ltd.
-
酒井 純一
Central Research Laboratories Sankyo Co. Ltd.
-
長野 光男
Central Research Laboratories Sankyo Co. Ltd.
-
西村 卓三
Central Research Laboratories Sankyo Co. Ltd.
関連論文
- Quantitative Structure-activity Relationships in Minor Tranquilizers Benzodiazepinooxazole Derivatives
- Synthesis of Anomeric Pyrimidine Nucleoside 5'-Phosphates of L-Ribose, α-D-Cytidine 5'-Phosphate and 3-β-L-Ribofuranosyladenine 5'-Phosphate
- Uber Tetrodotoxin. VI. Mitteilung. 2-Amino-6-methylchinazolin als Abbauprodukt von Tetrodotoxin.
- Uber Tetrodotoxin. Mitteilung. Synthese des C_9-Base-methylathers.
- Uber Tetrodotoxin. IV. Mitteilung. Die Struktur der C_9-Base, die sich durch Einwirkung der Alkalilauge auf Tetrodotoxin gewinnen la■t.
- 6.テトロドトキシンの構造研究
- Uber die Struktur der C_9-Base, die sich durch Behandlung mit Alkalilauge aus Tetrodotoxin gewinnen laβt
- Studies on Seven-membered Ring Compounds. XXIII. Reactions of Tropylium Ions Having Fused Heterocyclic System with Various Amines
- Studies on Seven-membered Ring Compounds. XXII. Preparation of Tropylium Ions Having Fused Heterocyclic Systems
- Studies on Seven-membered Ring Compounds. XIX. Reactions of Troponeimine Derivatives. (1)
- Studies on Seven-membered Ring Compounds. XV. Preparations of Troponeimine Derivatives
- Synthesis of α-Amino-cycloheptatriene-1-acetic Acids and Their 7-Acylaminocephalosporin Derivatives
- Synthesis of Amino Acid and 4,5-Dihydro-6H-1,3-thiazine Derivatives for the Preparation of Cephalosporin Compounds
- 3-Trifluoromethylcephalosporins. II. Synthesis and in Vitro Antibacterial Activities of 3-Trifluoromethylcephalosporin Derivatives
- 3-Trifluoromethylcephalosporins. I. Total Synthesis of tert-Butyl (±)-7-Amino-3-trifluoromethyl-3-cephem-4-carboxylate
- Syntheses of Highly Antibacterial 3-Vinylcephalosporin Derivatives
- Studies on Anticoccidial Agents. VII. An Improved Synthesis of α^4-Norpyridoxol
- Studies on Seven-membered Ring Compounds. XXXVI. Synthesis of Azulene Derivatives by Ring Closure of β-Cycloheptatrienyl-substituted Carbonyl Compounds
- Studies on Seven-membered Ring Compounds. XXXV. Ring Closure of γ-Cycloheptatrienyl-substituted α, β-Unsaturated Carbonyl Compounds to Benzocycloheptene Derivatives
- Studies on Seven-membered Ring Compounds. XXXIV. Reactions between Tropylium Cation and Dienamines
- Studies on Seven-membered Ring Compounds. XXXIII. Reactions between Tropylium Cation and Enamines
- Design of New Antidepressants, 4-Anilinopyrimidine Derivatives, Based on Quantitative Structure-Activity Relationships(Medicinal Chemistry,Chemical)
- A Method for Calculation of the Aqueous Solubility of Organic Compounds by Using New Fragment Solubility Constants
- Reactions of Ethyl 2-(1-Indanylidene) cyanoacetate Anion with Alkylating Agents and Aldehydes
- Studies on Quinolizinium Salts. IX. Ring-Opening Reactions of Benzo [α]-and Benzo [c] quinolizinium Bromides with a Grignard Reagent and Geometrical Determinations of the Resultant Butadienes
- Reactions of Chlordiazepoxide and Diazepam N-Oxide with Dimethyl Acetylenedicarboxylate with Rearrangement to Quinoxaline Derivatives and X-Ray Analysis of a Resultant Tetracyclic Compound
- Optical Inversion of (2R)-to (2S)-Isomers of 2-[4-(2-Oxocyclopentylmethyl)-phenyl] propionic Acid (Loxoprofen), a New Anti-inflammatory Agent, and Its Monohydroxy Metabolites in the Rat
- Studies on Benzodiazepinooxazoles. II. Crystal and Molecular Structure of 10-Bromo-2,3,5,6,7,11b-hexahydro-2-methyl-11b-phenylbenzo [6,7]-1,4-diazepino [5,4-b] oxazol-6-one, C_H_O_2N_2Br・C_2H_5OH
- Synthesis of a Tricyclic Benzodiazepine Derivative from Chlordiazepoxide and X-Ray Crystallographic Analysis of a Rearrangement Product, the Indolenine Derivative
- 有機イオウ化合物に関する研究(第15報)脱硫閉環反応におけるプロトンならびに重金属イオンの役割
- Studies on Organo Sulfur Compounds. VII. The Reaction Mechanism of 4-Benzylidene-1,3-oxathiolane-2-thione and Metal Xanthates
- Studies on Organo Sulfur Compounds. VI. The Reaction of S-Methyl-O-α-acetylenyl Xanthates and Metal Xanthates
- Studies on Organo Sulfer Compound. V. The Reaction of 4-Alkylidene-1,3-oxathiolane-2-thiones and Metal Xanthate
- Studies on Organo Sulfur Compounds. IV. The Reaction of Sodium sec- and tert-α-Acetylenyl Xanthates with Alkyl Halide
- Studies on Organo Sulfur Compounds. III. The Reaction of Sodium prim-α-Acetylenyl Xanthates and Alkyl Halide
- Studies on Organo Sulfur Compounds. II. The Reaction of sec- and tert-α-Acetylenic Alcohols and Carbon Disulfide
- Studies on Organo Sulfur Compound. I. The Reaction of Prim. α-Acetylenic Alcohols and Carbon Disulfide
- Reactions of 2-Piperidylacetohydrazides with Ethyl Acetoacetate or Acetylenic Acid Esters. Formation of 3,4-Dimethylpyrano-[2,3-c] pyrazol (6) ones and Perhydropyrazolo [2,3-a]-pyrido [1,2-c] pyrimidin-2,5-diones
- Studies on Benzodiazepinooxazoles. V. Reactions of Benzo [6,7]-1,4-diazepino [5,4-b] oxazole Derivatives with Acetic Anhydride
- Studies on Benzodiazepinooxazoles. IV. The Formation of Quinolones by the Ring Contraction of a Benzo [6,7]-1,4-diazepino [5,4-b]-oxazole Derivative
- Studies on Benzodiazepinooxazoles. III. Reactions and Rearrangements of Benzo [6,7]-1,4-diazepino-[5,4-b] oxazole Derivatives
- Studies on Organic Sulfur Compounds. XIV. The Reaction of N-Alkoxy-carbonyl-N'-(2-thiazolyl) thioureas with Some Oxidants
- Syntheses of 2-Hydroxymethylnicotinic Acid Lactone, 2-Hydroxymethylpyridine-3-acetic Acid Lactone, and Some of their Derivatives
- Synthesis of 5-Hydroxymethylquinoline-4-carboxylic Acid Lactone.
- Studies on Organic Sulfur Compounds. XVI. Nucleophilic Reaction of Heterocyclic Bases with Alkoxycarbonyl Isothiocyanates
- Studies on Organic Sulfur Compounds. XIII. The Oxidation Reaction of Alkoxycarbonylthioureas with Bromine
- 有機イオウ化合物に関する研究(第12報)o-置換芳香族チオアロファン酸エステルの脱硫閉環反応について
- Studies on Organic Sulfur Compounds.XI.Synthesis of 2-Alkylthio-thiazolo[3,2-α]-s-triazine-4-ones
- Studies on Organic Sulfur Compounds.X. The Reactions of Alkoxycarbonyl Isothiocyanates with prim-α-Acetylenic Alcohols
- Studies on Organic Sulfur Compounds. IX. The Reaction of Ethoxycarbonyl Isothiocyanate with 4,5-Substituted 2-Aminothiazoles
- Studies on Organic Sulfur Compounds. VIII. The Reaction of Alkoxycarbonyl Isothiocyanates and 2-Aminothiazole
- Studies on Organic Sulfur Compounds. XVII. Ambident Reactivities of Alkoxycarbonyl Isothiocyanates with Heterocyclic Bases
- Synthesis of N^6- or 8-Substituted 9-(β-D-Arabinofuranosyl)-adenines and Their Antiviral Activities against Herpes Simplex and Vaccinia Viruses
- Studies on Synthetic Nucleotides. I. A Convenient Synthesis of Ribonucleotides.
- Studies on Synthetic Nucleosides V. Anomeric Pyrimidine Nucleosides of D-Arabinose and D-Lyxose
- A Convenient Synthesis of Nucleotides
- Studies on Synthetic Nucleosides. IV. A New Synthetic Method of Pyrimidine and Purine Ribosides
- Studies on Synthetic Nucleosides. I. Trimethylsilyl Derivatives of Pyrimidines and Purines.
- A New Synthetic Method of Nucleosides
- The Studies on Quinolizinium Salts. II. Ring Opening Reactions of Quinolizinium Bromide by Grignard Reagents
- The Studies on Quinolizinium Salts. I. Syntheses of Quinolizinium and 1-, 2-, 3-, and 4-Methylquinolizinium Bromides
- Studies on Quinolizinium Salts. III. Ring Opening Reactions of Monomethylquinolizinium Bromides by Phenylmagnesium Bromide