CAS: 147030-48-6; 2-(2,6-Diiodo-4-((2-Methylbenzofuran-3-yl)Methyl)Phenoxy)Acetic Acid

上下游产品

2,6-二碘-4-[(2-甲基-1-苯并呋喃-3-基)甲基]苯酚 2-Methyl-3-(3,5-Diiodo-4-Hydroxybenzyl)Benzofuran 401917-61-1
2-[4-(2-丁基-1-苯并呋喃-3-羰基)-2,6-二碘苯氧基]乙酸 2-N-Butyl-3-(3,5-Diiodo-4-Carboxymethoxy-Benzoyl)Benzofuran 147030-47-5
(4-羟基-3,5-二碘苯基)(2-甲基-1-苯并呋喃-3-基)甲酮 2-Methyl-3-(3,5-Diiodo-4-Hydroxybenzoyl)Benzofuran 10402-56-9
(4-甲氧基苯基)(2-甲基-1-苯并呋喃-3-基)甲酮 2-Methyl-3-(4'-Methoxybenzoyl)Benzofuran 94541-06-7

📜(4-甲氧基苯基)(2-甲基-1-苯并呋喃-3-基)甲酮置于吗啉,Sodium Hydroxide,Sodium Tetrahydroborate,Tetramethylammonium Dichloroiodate,吡啶盐酸盐,Potassium Carbonate,Zinc(II) Iodide体系中,用 甲醇,1,2-二氯乙烷,N,N-二甲基甲酰胺 用作溶剂,化学反应 7.75H,反应生成{2,6-二碘-4-[(2-甲基-1-苯并呋喃-3-基)甲基]苯氧基}乙酸
参考文献:Synthesis And Preliminary Characterization Of A Novel Antiarrhythmic Compound (Kb130015) With An Improved Toxicity Profile Compared With Amiodarone
标题:Synthesis And Preliminary Characterization Of A Novel Antiarrhythmic Compound (Kb130015) With An Improved Toxicity Profile Compared With Amiodarone
摘要:Recent Developments In Antiarrhythmic Therapy Have Indicated That The Best Approach To Pharmacologically Controlling Supraventricular Arrhythmias And Life-Threatening Ventricular Tachyarrhythmias Is By Prolonging Cardiac Repolarization Rather Than By Blocking Conduction. In This Context,Amiodarone Has Emerged As The Most Potent Compound,But Its Universal Use Has Been Limited By Its Toxicity Profile. There Are Data To Suggest That An Important Component Of Amiodarones Antiarrhythmic Action Might Be Mediated Via Inhibition Of Thyroid Hormone Action In The Heart. Therefore,A New Series Of Carboxymethoxybenzoyl And Benzyl Derivatives Of Benzofuran Has Been Prepared And Evaluated As Thyroid Hormone Receptor Antagonists. Within This Series,2-Methyl-3-(3,5-Diiodo-4-Carboxymethoxybenzyl)Benzofuran Kb130015 (7) Was Found To Reveal The Most Promising In Vitro Data. It Inhibits The Binding Of I-125-T-3 To The Human Thyroid Hormone Receptors (Hthr) Alpha(1) And Beta(1). T-3-Antagonism Was Confirmed In Reporter Cell Assays Employing Chokl Cells (Chinese Hamster Ovary Cells) Stably Transfected With Hthralpha(1) Or Hthrbeta(1) And An Alkaline Phosphatase Reporter Gene Downstream A Thyroid Response Element. The Derived Ic50 Values Were 2.2 Mum For Hthralpha(1) And 4.1 Mum For Hthrbeta(1). Compound 7 Was Selected For Further Characterization Of Chronic Effects On Ventricular Papillary Muscle By Transmembrane Electrophysiology After Daily Intraperitoneal Injection Of The Ligand (40 Mg/kg Body Weight) In Guinea Pigs. Compound 7 Was Found To Prolong The Action Potential Duration At 90% (Apd(90)) Repolarization Time (219 +/-22 Ms,Control: 186 +/-9 Ms,P < 0.01) Without Exhibiting Any Reverse-Rate Dependency Of Action In A Manner Similar To That Of Amiodarone. In General,Preliminary Tolerance Experiments With 7 Demonstrated An Improved Safety Profile Compared To That Of Amiodarone. In Summary,7 Appears To Be Less Toxic Than Amiodarone While Maintaining Its Electrophysiologic Properties Consistent With Antiarrhythmic Activity. Its Potential Antiarrhythmic Actions Warrant Further Investigations.
Doi:10.1021/jm001126+