[The search for new antiparasitic agents. 10. The synthesis, toxicological and antimalarial properties of nitrogen-containing heterocycles with a 4-(4-alkylpiperazinyl-1) phenylamine substituent (the preparation quinoprazine)].
Synthesis is described and acute toxicity and antimalaria action is studied in new derivatives of quinoline and benzo(g)quinoline containing a 4-(4-alkylpiperazinyl-1)phenylamine substitute. Only the derivatives of benzo(g)quinoline were found to have a high antimalaria effect and to have advantages over the standard agent chloroquine on their tolerance and protective action. One of the compounds, 4-[4-(4-ethylpiperazinyl-1)phenylamino] benzo(g)quinoline, named QUINOPRAZINE, showed some action against Plasmodium berghei chloroquine--resistant infection (isolate LN-K65). This agent was elected for further tests.
Mikhaĭlitsyn
F S
FS
Kozyreva
N P
NP
Rabinovich
S A
SA
Maksakovskaia
E V
EV
Kulikovskaia
I M
IM
Dadasheva
N R
NR
Lebedeva
M N
MN
Bekhli
A F
AF
Lychko
N D
ND
Uvarova
N A
NA
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000627:therapeutic use / Q000633:toxicity; D002738:Chloroquine / Q000031:analogs & derivatives / Q000627:therapeutic use; D004353:Drug Evaluation, Preclinical; D005260:Female; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000627:therapeutic use / Q000633:toxicity; D008288:Malaria / Q000188:drug therapy; D008297:Male; D051379:Mice; D010962:Plasmodium berghei; D011804:Quinolines / Q000138:chemical synthesis* / Q000627:therapeutic use / Q000633:toxicity
D000962:Antimalarials; D006571:Heterocyclic Compounds; D011804:Quinolines; C076268:quinoprazine; C023676:chloroquine diphosphate; D002738:Chloroquine
Izyskanie novykh protivoparazitarnykh sredstv. 10. Sintez, toksikologicheskkie i protivomaliariĭnye svoĭstva nekotorykh azotsoderzhashchikh geterotsiklov s 4-(4-alkilpiperazinil-1)fenilaminnym zamestitelem (preparat khinoprazin).