The present invention discloses a
thrombolysis oligopeptide-
imidazolidine binary conjugate, a preparation method and uses thereof. According to the present invention, L-Lys is adopted as a linking arm to link 1,3-dioxy-2-[(4-oxyacetic acid)phenyl]-4,4,5,5-tetramethylimidazoline, ARPAK having a
thrombolysis effect, GRPAK, RPAK or PAK to obtain the
thrombolysis oligopeptide-
imidazolidine binary conjugate represented by a formula I or II, wherein the thrombolysis
oligopeptide-
imidazolidine binary conjugate integrally has characteristics of nanometer structure, BBB crossing, thrombolysis and NO removing. The thrombolysis oligopeptide-imidazolidine binary conjugate has high NO free radical clearance activity, excellent thrombolysis activity and excellent antithrombosis activity.
In vivo anti-
stroke activity test results show that: with the thrombolysis oligopeptide-imidazolidine binary conjugate, nerve functions of
stroke rats can be effectively protected, brain
infarct volume of the
stroke rats can be reduced, excellent anti-stroke activity is provided, and the thrombolysis oligopeptide-imidazolidine binary conjugate can be prepared into a clinical
drug for brain
infarction treatment.