CAS: 57719-81-0; 11-Hydroxy-4,11B-Dimethyl-8-Methylene-7-Oxotetradecahydro-6A,9-Methanocyclohepta[a]Naphthalene-4-Carboxylic Acid

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ent-11α,15α-Dihydroxykaur-16-en-19-oic acid

📜Ent-11α,15α-Dihydroxykaur-16-En-19-Oic Acid置于2,2,6,6-四甲基哌啶氧化物,碘苯二乙酸,溶剂黄146体系中,用 乙腈 作为反应溶剂,化学反应 6.0H,以5 Mg的收率获得产物(4Alpha,11Beta)-11-羟基-15-氧代贝壳杉-16-烯-18-酸
参考文献:Discovery And Structure-activity Relationships Of Ent-Kaurene Diterpenoids As Potent And Selective 11β-Hsd1 Inhibitors: Potential Impact In Diabetes
标题:Discovery And Structure-activity Relationships Of Ent-Kaurene Diterpenoids As Potent And Selective 11β-Hsd1 Inhibitors: Potential Impact In Diabetes
摘要:The Biological Screening Of A Collection Of Nature occurring Diterpenoids Against 11 Beta-Hsd1 Resulted In The Discovery Of The Lead Compound 1B,Which Pointed To The Therapeutic Potential For Type 2 Diabetes. Subsequently,An Optimization Project Was Initiated. Starting From Compound 1B And Its Counterpart 2,The Hemi-Synthesis Was Performed On Kaurenic Acid Scaffolds Yielding 36 Derivatives. Further Evaluations On Both Human And Mouse 11 Beta-Hsd Revealed That Seven Urea Derivatives Exhibited Significant Improved Potency And Selectivity. Especially,The Urea 19A Has An Ic50 (Human 11 Beta-Hsd1) = 9.4 Nm And Selectivity Index (Human 11 Beta-Hsd) > 10,649. The 2D And 3D Binding Models Of The Complex 19A/11 Beta-Hsd1 Were Generated Using Docking Simulations. Based On The Results,The Structural Activity Relationships (Sars) Of Compounds 1B And 2 Were Also Discussed. (C) 2013 Elsevier Masson Sas. All Rights Reserved.
DOI:10.1016/j.Ejmech.2013.05.010