Gb. Barlin et al., POTENTIAL ANTIMALARIALS .18. SOME MONO-MANNICH AND DI-MANNICH BASES OF 3-[7-CHLORO(AND TRIFLUOROMETHYL)QUINOLIN-4-YLAMINO]PHENOL, Australian Journal of Chemistry, 46(11), 1993, pp. 1685-1693
Syntheses are reported for mono- and di-Mannich base derivatives of 3-
[7-chloro(and trifluoromethyl)quinolin-4-ylamino]phenols by Mannich re
action on 3-[7-chloro(and trifluoromethyl)-quinolin-4-ylamino]phenols
or by condensation of Mannich base derivatives of 3-aminophenol, prepa
red from 3-nitrophenol, with the appropriate 4-chloroquinoline. The an
timalarial activity of in-4'-ylamino)-2,6-bis[pyrrolidin-1''-ylmethyl-
(or piperidin-1''-ylmethyl)]phenol against the Fc-27 isolate of Plasmo
dium falciparum was comparable to that of chloroquine, and it was not
significantly diminished in tests against the chloroquine-resistant K-
1 isolate.