Gb. Barlin et al., POTENTIAL ANTIMALARIALS .21. MANNICH BASE DERIVATIVES OF 4-[7-CHLORO(AND 7-TRIFLUOROMETHYL)QUINOLIN-4-YLAMINO]PHENOLS, Australian Journal of Chemistry, 47(8), 1994, pp. 1553-1560
Syntheses are reported for lin-4-ylamino)-2,6-bis(piperidin-1-ylmethyl
)phenol (2) and its 3-fluoro and 3-piperidinyl derivatives. Some mono-
Mannich analogues with 2-fluoro, 2-t-butyl and 3-trifluoromethyl subst
ituents have also been prepared. In tests for antimalarial activity ag
ainst the FC-27 and K-1 isolates of Plasmodium falciparum in vitro, co
mpound (2) proved to be the most active (IC50 6.3-12.5 nm).