Based on the antiplatelet aggregation mechanism and the bioisosterism principle of the reference drug picotamide, thirteen novel derivatives of arylamide and arylsulfonamide were designed and prepared. The biological ...Based on the antiplatelet aggregation mechanism and the bioisosterism principle of the reference drug picotamide, thirteen novel derivatives of arylamide and arylsulfonamide were designed and prepared. The biological activities of these derivatives were investigated. The chemical structures of the target compounds were confirmed by ^1H NMR and IR. The in vitro activities of antiplatelet aggregation of the thirteen target compounds were assessed by Bore＇s method. Compounds 2b and 8h have significant antiplatelet aggregation activities, which are superior to the corresponding activity of Picotamide.展开更多
N,N,N＇,N＇-Tetrabromobenzene-1,3-disulfonamide （TBBDA）/triphenylphosphine and N,N,N＇,N＇-tetra- chlorobenzene-1,3-disulfonamide （TCBDA）/triphenylphosphine have been introduced as highly efficient systems for the...N,N,N＇,N＇-Tetrabromobenzene-1,3-disulfonamide （TBBDA）/triphenylphosphine and N,N,N＇,N＇-tetra- chlorobenzene-1,3-disulfonamide （TCBDA）/triphenylphosphine have been introduced as highly efficient systems for the versatile conversion of aldoxime derivatives into nitriles. The process reported here is operationally simple and reactions have been mildly performed in dichloromethane at room temperature.展开更多
文摘Based on the antiplatelet aggregation mechanism and the bioisosterism principle of the reference drug picotamide, thirteen novel derivatives of arylamide and arylsulfonamide were designed and prepared. The biological activities of these derivatives were investigated. The chemical structures of the target compounds were confirmed by ^1H NMR and IR. The in vitro activities of antiplatelet aggregation of the thirteen target compounds were assessed by Bore＇s method. Compounds 2b and 8h have significant antiplatelet aggregation activities, which are superior to the corresponding activity of Picotamide.
基金Bu-Ali Sina University, Center of Excellence and Development of Chemical Methods (CEDCM) for fnancial support
文摘N,N,N＇,N＇-Tetrabromobenzene-1,3-disulfonamide （TBBDA）/triphenylphosphine and N,N,N＇,N＇-tetra- chlorobenzene-1,3-disulfonamide （TCBDA）/triphenylphosphine have been introduced as highly efficient systems for the versatile conversion of aldoxime derivatives into nitriles. The process reported here is operationally simple and reactions have been mildly performed in dichloromethane at room temperature.
