Synthesis and antiprotozoal activities of some new triazine derivatives including a new antitrypanosomal agent: SIPI-1029.
Two series of compounds, 1,2-dihydro-2,2-dimethyl-4, 6-diamino-1-(omega-haloalkyloxy)-s-triazines and O, O'-bis (4, 6-diamino-1, 2-dihydro-2, 2-disubstituted-s-triazin-l-yl) alkanediols were synthesized and tested against Plasmodium berghei and Trypanosoma evansi in mice. Most title compounds showed good antimalarial activity and compounds IIc-e showed 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.
Zhou
W C
WC
Shanghai Institute of Pharmaceutical Industry.
Xin
Z M
ZM
Zhang
X P
XP
Shen
J
J
Qiu
Q P
QP
D000818:Animals; D002417:Cattle; D002418:Cattle Diseases / Q000188:drug therapy / Q000469:parasitology; D051379:Mice; D051381:Rats; D014227:Triazines / Q000138:chemical synthesis* / Q000627:therapeutic use / Q000633:toxicity; D014344:Trypanocidal Agents / Q000138:chemical synthesis* / Q000627:therapeutic use / Q000633:toxicity; D014352:Trypanosomiasis / Q000188:drug therapy / Q000662:veterinary
D014227:Triazines; D014344:Trypanocidal Agents; C115203:trybizine