New Ethacrynic Acid Derivatives as Potent Cytoskeletal Modulators in Trabecular Meshwork Cells(Medicinal Chemistry)
スポンサーリンク
概要
- 論文の詳細を見る
A series of ethacrynic acid (ECA) derivatives were synthesized and examined for ocular hypotensive activity. Efficacy was evaluated in a cell-shape assay, using human trabecular meshwork cells, and cytotoxicity in a (3-(4,5-dimethylthiazole-2-yl)-5-(3-carboxymethoxy phenyl)-2-(4-sulfophenyl)-2H-tetrazolium) assay, using cultured bovine trabecular meshwork cells. Many of the derivatives demonstrated efficacy equal to or greater than that of ECA. SA9000 was selected as the most promising candidate for a novel ocular hypotensive drug with few side effects.
- 公益社団法人日本薬学会の論文
- 2004-06-01
著者
-
Epstein David
Department Of Ophthalmology Duke University Medical Center & Health System
-
Epstein David
参天製薬奈良研究開発センター
-
Ichikawa M
Healthcare Research Institute Wakunaga Pharmaceutical Co. Ltd.
-
Hara Hideaki
Research And Development Center Santen Pharmaceutical Co. Ltd.
-
SHIMAZAKI Atsushi
Research and Development Center, Santen Pharmaceutical Co., Ltd.
-
RAO Ponugoti
Department of Ophthalmology, Duke University Medical Center & Health System
-
MATSUGI Takeshi
Research and Development Center, Santen Pharmaceutical Co., Ltd.
-
ICHIKAWA Masaki
Research and Development Center, Santen Pharmaceutical Co., Ltd.
-
SUHARA Hiroshi
Research and Development Center, Santen Pharmaceutical Co. Ltd.
-
KONOMI Koji
Research and Development Center, Santen Pharmaceutical Co. Ltd.
-
TAKAGI Yasutaka
Research and Development Center, Santen Pharmaceutical Co. Ltd.
-
Rao Ponugoti
Department Of Ophthalmology Duke University Medical Center & Health System
-
Konomi Koji
Research And Development Center Santen Pharmaceutical Co. Ltd.
-
Suhara Hiroshi
Research And Development Center Santen Pharmaceutical Co. Ltd.
-
Takagi Yasutaka
Research And Development Center Santen Pharmaceutical Co. Ltd.
-
Matsugi Takeshi
Research And Development Center Santen Pharmaceutical Co. Ltd.
-
Shimazaki Atsushi
Research And Development Center Santen Pharmaceutical Co. Ltd.
-
Hara H
(present Address)corporate Planning Dept. Yamanouchi Pharmaceutical Co. Ltd.
-
Ichikawa Masaki
Research And Development Center Santen Pharmaceutical Co. Ltd.
関連論文
- 2-(3-Pyridyl)thiazolidine-4-carboxamide Derivatives. II. Structure-Activity Relationships and Active Configuration of 2-(3-Pyridyl)thiazolidine-4-carboxamides as Platelet-Activating Factor Receptor Antagonists
- 2-(3-Pyridyl)thiazolidine-4-carboxamides. 1. Novel Orally Active Antagonists of Platelet-Activating Factor (PAF)
- Realizing Visual Functions with the Reaction-Diffusion Mechanism
- Effect of Various Halide Salts on the Incompatibility of Cyanocobalamin and Ascorbic Acid in Aqueous Solution
- Pharmacokinetic Study of Allixin, a Phytoalexin Produced by Garlic
- HPLC Determination of (+)-Pseudoephedrine and (-)-Ephedrine in Japanese Herbal Medicines Containing Ephedra Herb Using Solid-Phase Extraction
- Effects of the New Ethacrynic Acid Oxime Derivative SA12590 on Intraocular Pressure in Cats and Monkeys(Pharmacology)
- Effects of Novel Ethacrynic Acid Derivatives on Human Trabecular Meshwork Cell Shape, Actin Cytoskeletal Organization, and Transcellular Fluid Flow(Pharmacology)
- Effects of the New Ethacrynic Acid Derivative SA9000 on Intraocular Pressure in Cats and Monkeys(Pharmacology)
- New Ethacrynic Acid Derivatives as Potent Cytoskeletal Modulators in Trabecular Meshwork Cells(Medicinal Chemistry)
- Characterization of Ocular Pharmacokinetics of Tilisolol after Instillation into Anesthetized Rabbits
- Topical Delivery System of Ophthalimic Drugs by Periocular Injection with Viscous Solution
- Drug Absorption Behavior after Periocular Injections
- Studies on Tetrahydroisoquinolines. XXXI. : A synthesis of Tetrahydroisoquinoline Dimers by Intermolecular C-O Coupling
- In Vitro Characteristics and in Vivo Plasma Disposition of Cisplatin Conjugated with Oxidized and Dicarboxymethylated Dextrans
- SYNTHESIS OF VALPROYL-2-PYRROLIDINONE AND ITS EVALUATION AS A COGNITIVE DRUG WITH THE ABILITY TO MODULATE ACIDIC AMINO ACIDS IN THE BRAIN
- Determination of γ-Aminobutyric Acid and Associated Amino Acids in Mouse Brain by Liquid Chromatography
- A Novel Class of Inhibitors for Human Steroid 5α-Reductase : Synthesis and Biological Evaluation of Indole Derivatives. II
- A Novel Class of Inhibitors for Human Steroid 5α-Reductase : Phenoxybenzoic Acid Derivatives. I
- 2-(3-Pyridyl)thiazolidine-4-carboxamide Derivatives. III. Synthesis of Metabolites and Metabolism of 2-(3-Pyridyl)thiazolidine-4-carboxamides YM461 and YM264 as Platelet-Activating Factor (PAF) Receptor Antagonists
- A Novel Class of Inhibitors for Human and Rat Steroid 5α-Reductases : Synthesis and Biological Evaluation of Indoline and Aniline Derivatives. III
- Effects of Topically Instilled Bunazosin Hydrochloride and Other Ocular Hypotensive Drugs on Endothelin-1-induced Constriction in Rabbit Retinal Arteries
- Agarwood Induced Laxative Effects via Acetylcholine Receptors on Loperamide-Induced Constipation in Mice
- New Fluoroprostaglandin F_ Derivatives with Prostanoid FP-Receptor Agonistic Activity as Potent Ocular-Hypotensive Agents (Pharmacology)
- Role of Oxidative Stress in Retinal Photoreceptor Cell Death in N-Methyl-N-nitrosourea-Treated Mice
- Identification of Phenolic Compounds in Aquilaria crassna Leaves Via Liquid Chromatography-Electrospray Ionization Mass Spectroscopy