[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)].

Abstract

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.

• Authors: F S Mikhaĭlitsyn, N P Kozyreva, S A Rabinovich, E V Maksakovskaia, I M Kulikovskaia, N R Dadasheva, M N Lebedeva, A F Bekhli, N D Lychko, N A Uvarova
• Journal: Meditsinskaia parazitologiia i parazitarnye bolezni (Med Parazitol (Mosk)) 1992 Jan-Feb Issue 1 Pg. 50-3 ISSN: 0025-8326 [Print] Russia (Federation)
• Vernacular Title: Izyskanie novykh protivoparazitarnykh sredstv. 10. Sintez, toksikologicheskkie i protivomaliariĭnye svoĭstva nekotorykh azotsoderzhashchikh geterotsiklov s 4-(4-alkilpiperazinil-1)fenilaminnym zamestitelem (preparat khinoprazin).
• PMID: 1508078 (Publication Type: Comparative Study, English Abstract, Journal Article)

Chemical References

• Antimalarials
• Heterocyclic Compounds
• Quinolines
• quinoprazine
• chloroquine diphosphate
• Chloroquine

Topics

• Animals
• Antimalarials (chemical synthesis, therapeutic use, toxicity)
• Chloroquine (analogs & derivatives, therapeutic use)
• Drug Evaluation, Preclinical
• Female
• Heterocyclic Compounds (chemical synthesis, therapeutic use, toxicity)
• Malaria (drug therapy)
• Male
• Mice
• Plasmodium berghei
• Quinolines (chemical synthesis, therapeutic use, toxicity)