[Synthesis of 4-methyl-5-substituted phenoxy-primaquine analogues and preliminary evaluation on their antimalarial activity].
On basis of our previous work, seven 4-methyl-5-substituted phenoxy-6-methoxy-8-(1-methyl-4-amino-butylamino)-quinolines (II2-8) were synthesized and their antimalarial activities were preliminarily evaluated. The target compounds were prepared from 2-nitro-4-methoxy-5-bromo-acetanilide as previously described. The structures of II2-8 and all of the unknown intermediates were confirmed by elementary and spectral analyses. Preliminary biological evaluation revealed that all of II2-8 exhibited significant blood schizonticidal activity and were 4-8 times as effective as primaquine in causal prophylactic test in mice.
Institute of Microbiology and Epidemiology, Academy of Military Medical Science, Beijing.
B H
BH
Zhong
R X
RX
Deng
Y L
YL
Shi
G F
GF
Li
J X
JX
Zhong
J D
JD
Yang
J
J
Wang
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000627:therapeutic use; D008288:Malaria / Q000188:drug therapy; D051379:Mice; D010962:Plasmodium berghei; D011319:Primaquine / Q000138:chemical synthesis* / Q000627:therapeutic use
D000962:Antimalarials; D011319:Primaquine