CAS: 175137-62-9; 2-(Thiophen-2-Ylsulfonyl)Acetonitrile

📜Thiophene-2-Thioacetonitrile置于间氯过氧苯甲酸体系中,用 二氯甲烷 用作溶剂,化学反应 2.0H,反应生成噻吩-2-磺酰乙腈
参考文献:Nanomolar Potency And Metabolically Stable Inhibitors Of Kidney Urea Transporter Ut-B
标题:Nanomolar Potency And Metabolically Stable Inhibitors Of Kidney Urea Transporter Ut-B
摘要:Urea Transporters,Which Include Ut-B In Kidney Microvessels,Are Potential Targets For Development Of Drugs With A Novel Diuretic ('Urearetic') Mechanism. We Recently Identified,By High-Throughput Screening,A Triazolothienopyrimidine Ut-B Inhibitor,1,That Selectively And Reversibly Inhibited Urea Transport With Ic50 = 25.1 Nm And Reduced Urinary Concentration In Mice (Yao Et Al. J. Am. Soc. Nephrol.,In Press). Here,We Analyzed 273 Commercially Available Analogues Of 1 To Establish A Structure-Activity Series And Synthesized A Targeted Library Of 11 Analogues To Identify Potent,Metabolically Stable Ut-B Inhibitors. The Best Compound,{3-[4-(1,1-Difluoroethyl)Benzenesulfonyl]Thieno[2,3-E][1,2,3]Triazolo[1,5-A]Pyrimidin-5-Y1}Thiophen-2-Ylmethylamine,3K,Had Ic50 Of 23 And 15 Nm For Inhibition Of Urea Transport By Mouse And Human Ut-B,Respectively,And Similar To 40-Fold Improved In Vitro Metabolic Stability Compared To 1. In Mice,3K Accumulated In Kidney And Urine And Reduced Maximum Urinary Concentration. Triazolothienopyrimidines May Be Useful For Therapy Of Diuretic-Refractory Edema In Heart And Liver Failure.
Doi:10.1021/jm300491Y