Based on the EDRF(endothelium derived relaxing factor)-like effects for polyarginine Arg-Arg-oH was selected as the lead compound and its derivatives Arg-Arg- OCH_3.Arg Arg-Arg-OH,HO-ArgCOCH_2CH_2COArg-OH,HO-ArgCOCH_2...Based on the EDRF(endothelium derived relaxing factor)-like effects for polyarginine Arg-Arg-oH was selected as the lead compound and its derivatives Arg-Arg- OCH_3.Arg Arg-Arg-OH,HO-ArgCOCH_2CH_2COArg-OH,HO-ArgCOCH_2COArg-OH,were synthesized.These substances showed on bioassay various degrees of vasorelaxant activities. With protection for the C-terminal of Arg-Arg-OH with a methyl ester.the vasorelaxing ac- tivitv was decreased.In contrast.when the N-terminal of Arg-OH was protected with mal- onic acid or butane diacid.the biological activites were lower than those of Arg-Arg-OH due to the lowered metabolic rate.With protection of N-terminal of Arg-Arg-OH with L-Arg residue.Arg-Arg-Arg-OH was obtained,which showed a vasorelaxing activity better than that of Arg-Arg-OH.The bioactivities observed on the Wister's rats for the former com- pound become the experimental basis for prodrug design of EDRF.展开更多
基金This project was supported by the National Natural Science Foundation of China
文摘Based on the EDRF(endothelium derived relaxing factor)-like effects for polyarginine Arg-Arg-oH was selected as the lead compound and its derivatives Arg-Arg- OCH_3.Arg Arg-Arg-OH,HO-ArgCOCH_2CH_2COArg-OH,HO-ArgCOCH_2COArg-OH,were synthesized.These substances showed on bioassay various degrees of vasorelaxant activities. With protection for the C-terminal of Arg-Arg-OH with a methyl ester.the vasorelaxing ac- tivitv was decreased.In contrast.when the N-terminal of Arg-OH was protected with mal- onic acid or butane diacid.the biological activites were lower than those of Arg-Arg-OH due to the lowered metabolic rate.With protection of N-terminal of Arg-Arg-OH with L-Arg residue.Arg-Arg-Arg-OH was obtained,which showed a vasorelaxing activity better than that of Arg-Arg-OH.The bioactivities observed on the Wister's rats for the former com- pound become the experimental basis for prodrug design of EDRF.
