CAS: 220616-39-7; (3-(Cyanomethyl)Phenyl)Boronic Acid

📜3-氰基甲基苯基硼酸频哪醇酯置于二乙醇胺,盐酸,水体系中,用 乙醚,异丙醇,四氢呋喃 用作溶剂,化学反应 73.0H,以72.7%的收率获得3-氰基甲基苯基硼酸
参考文献:Mtb Pkna/pknb Dual Inhibition Provides Selectivity Advantages For Inhibitor Design To Minimize Host Kinase Interactions
标题:Mtb Pkna/pknb Dual Inhibition Provides Selectivity Advantages For Inhibitor Design To Minimize Host Kinase Interactions
摘要:Drug Resistant Tuberculosis (Tb) Infections Are On The Rise And Antibiotics That Inhibit Mycobacterium Tuberculosis Through A Novel Mechanism Could Be An Important Component Of Evolving Tb Therapy. Protein Kinase A (Pkna) And Protein Kinase B (Pknb) Are Both Essential Serine-Threonine Kinases In M. Tuberculosis. Given The Extensive Knowledge Base In Kinase Inhibition,These Enzymes Present An Interesting Opportunity For Antimycobacterial Drug Discovery. This Study Focused On Targeting Both Pkna And Pknb While Improving The Selectivity Window Over Related Mammalian Kinases. Compounds Achieved Potent Inhibition (K-I Approximate To 5 Nm) Of Both Pkna And Pknb. A Binding Pocket Unique To Mycobacterial Kinases Was Identified. Substitutions That Filled This Pocket Resulted In A 100-Fold Differential Against A Broad Selection Of Mammalian Kinases. Reducing Lipophilicity Improved Antimycobacterial Activity With The Most Potent Compounds Achieving Minimum Inhibitory Concentrations Ranging From 3 To 5 Mu M (1-2 Mu G/ml) Against The H37Ra Isolate Of M. Tuberculosis.
Doi:10.1021/acsmedchemlett.7B00239