WC Zhou, ZM Xin, XP Zhang, J Shen ,QPqiu, . SYNTHESIS AND ANTIPROTOZOAL ACTIVITIES OF SOME NEW TRIAZINE DERIVATIVES INCLUDING A NEW ANTITRYPANOSOMALAGENT:SIPI-1029J. Acta Pharmaceutica Sinica, 1996, 31(11): 823-830.
Citation: WC Zhou, ZM Xin, XP Zhang, J Shen ,QPqiu, . SYNTHESIS AND ANTIPROTOZOAL ACTIVITIES OF SOME NEW TRIAZINE DERIVATIVES INCLUDING A NEW ANTITRYPANOSOMALAGENT:SIPI-1029J. Acta Pharmaceutica Sinica, 1996, 31(11): 823-830.

SYNTHESIS AND ANTIPROTOZOAL ACTIVITIES OF SOME NEW TRIAZINE DERIVATIVES INCLUDING A NEW ANTITRYPANOSOMALAGENT:SIPI-1029

  • Two series of compound:1,2-dihydro-2,2-dirnethyl-4,6-diamino-1-(ω-haloakyloxy)-s-triazines and O,O'-bis(4,6-diamino-1,2-dihydro-2,2-disubstituted-s-triazin-1-yl)alkanediols were synthesised and tested against Plasmodium berghei and Trypanosoma evansi in mice.Most title compounds showed good antimalarial activity and compounds IIc~eshowed good antitrypanosomal effect.After further studies on pharmacology,toxicology,pharmacokinetics and efficacy on infected cattles compound IIe(SIPI-1029,T-46)was shown to be a new highly active antitrypanosomal agent with low toxicity and long half life in plasma.
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