📜3,4-二氯苯胺,二聚氰胺置于盐酸体系中,用 水 用作溶剂,化学反应 0.17H,反应生成1-(3,4-二氯苯基)双胍 盐酸盐
参考文献:Structural Insights Into The Development Of Cycloguanil Derivatives Astrypanosoma Bruceipteridine-Reductase-1 Inhibitors
标题:Structural Insights Into The Development Of Cycloguanil Derivatives Astrypanosoma Bruceipteridine-Reductase-1 Inhibitors
摘要:Cycloguanil Is A Known Dihydrofolate-Reductase (Dhfr) Inhibitor,But There Is No Evidence Of Its Activity On Pteridine Reductase (Ptr),The Main Metabolic Bypass To Dhfr Inhibition In Trypanosomatid Parasites. Here,We Provide Experimental Evidence Of Cycloguanil As An Inhibitor Of Trypanosoma Brucei Ptr1 (Tbptr1). A Small Library Of Cycloguanil Derivatives Was Developed,Resulting In 1 And 2A Having Ic50 Values Of 692 And 186 Nm,Respectively,Toward Tbptr1. Structural Analysis Revealed That The Increased Potency Of 1 And 2A Is Due To The Combined Contributions Of Hydrophobic Interactions,H-Bonds,And Halogen Bonds. Moreover,In Vitro Cell-Growth-Inhibition Tests Indicated That 2A Is Also Effective On T. Brucei. The Simultaneous Inhibition Of Dhfr And Ptr1 Activity In T. Brucei Is A Promising New Strategy For The Treatment Of Human African Trypanosomiasis. For This Purpose,1,6-Dihydrotriazines Represent New Molecular Tools To Develop Potent Dual Ptr And Dhfr Inhibitors.
Doi:10.1021/acsinfecdis.8B00358