[Synthesis of acridine derivatives of amino acid hydrazines and their antimalarial activity].
2-Methoxy-6-chloroacridine-9-yl- and 2-ethoxy-6-nitroacridine-9-yl-hydrazides of glycine, alpha- and beta-alanines, gamma-aminobutiric acid, epsilon-aminocaproic acid have been synthesized and their antimalarial activity has been investigated. The compounds were found to inhibit the growth of malaria parasite P. falciparum in in vitro cultures. Fifty per cent inhibitory concentrations ranged from 2 x 10(-7) to 6 x 10(-7) M and corresponded to therapeutic concentrations of known quinoline and acridine antimalarial drugs. The beta-alanine and gamma-aminobutiric acid derivatives were the most active and showed high activity against a chloroquine resistant strain of P. falciparum.
Shibnev
V A
VA
Finogenova
M P
MP
Grinberg
L N
LN
Allakhverdiev
A M
AM
D000166:Acridines / Q000138:chemical synthesis* / Q000494:pharmacology; D000596:Amino Acids / Q000138:chemical synthesis* / Q000494:pharmacology; D000962:Antimalarials / Q000138:chemical synthesis*; D055598:Chemical Phenomena; D002621:Chemistry; D006834:Hydrazines / Q000138:chemical synthesis* / Q000494:pharmacology; D007364:Intercalating Agents / Q000138:chemical synthesis*
D000166:Acridines; D000596:Amino Acids; D000962:Antimalarials; D006834:Hydrazines; D007364:Intercalating Agents
Sintez akridinovykh proizvodnykh gidrazidov aminokislot i ikh protivomaliariĭnaia aktivnost'.