CAS: 59804-25-0; Methyl 4-Hydroxy-2-Methyl-2H-Thieno[2,3-E][1,2]Thiazine-3-Carboxylate 1,1-Dioxide

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CAS号59804-24-9 methyl 3-[[N-[(... | CAS号98827-44-2 替诺昔康环合物 | CAS号74-88-4 碘甲烷 | CAS号59337-89-2 3-氯噻吩-2-羧酸 | CAS号59337-92-7 3-(氯磺酰)-2-噻吩羧酸甲酯 | CAS号59337-91-6 3-chlorosulfony... | CAS号59337-94-9 thieno[2,3-d]is... | CAS号106820-63-7 3-磺酰氨基乙酸甲酯-2-噻吩甲酸甲酯 | CAS号59804-37-4 替诺昔康

Methyl 2-(1,1,3-Trioxothieno[2,3-D][1,2]Thiazol-2-yl)Acetate置于甲醇,Sodium Hydroxide,Sodium Methylate体系中,用 乙醇,甲苯 作为反应溶剂,化学反应 28.0H,反应生成 2-甲基-4-羟基-2H-噻吩并[2,3-E]-1,2-噻嗪-3-甲酸甲酯-1,1-二氧化物
参考文献:Effect Of Structural Modification Of Enol−carboxamide-Type Nonsteroidal Antiinflammatory Drugs On Cox-2/cox-1 Selectivity
标题:Effect Of Structural Modification Of Enol−carboxamide-Type Nonsteroidal Antiinflammatory Drugs On Cox-2/cox-1 Selectivity
摘要:Meloxicam (5),An Nsaid In The Enol-Carboxamide Class,Was Developed On The Basis Of Its Antiinflammatory Activity And Relative Safety In Animal Models. In Subsequent Screening In Microsomal Assays Using Human Cox-1 And Cox-2,We Discovered That It Possessed A Selectivity Profile For Cox-2 Superior To Piroxicam And Other Marketed Nsaids. We Therefore Embarked On A Study Of Enol-Carboxamide Type Compounds To Determine If Cox-2 Selectivity And Potency Could Be Dramatically Improved By Structural Modification. Substitution At The 6-And 7-Positions Of The 4-Oxo-1,2-Benzothiazine-3-Carboxamide,Alteration Of The N-Methyl Substituent,And Amide Modification Were All Examined. In Addition We Explored Several Related Systems Including The Isomeric 3-Oxo-1,2-Benzothiazine-4-Carboxamides,Thienothiazines,Indolothiazines,Benzothienothiazines,Naphthothiazines,And 1,3-And 1,4-Dioxoisoquinolines. While A Few Examples Were Found With Greater Potency In The Cox-2 Assay,No Compound Tested Had A Better Cox-2/cox-1 Selectivity Profile Than That Of 5.
DOI:10.1021/jm9607010