Potential Antimalarials. XXI. Mannich Base Derivatives of 4-[7-Chloro(and 7-trifluoromethyl)quinolin-4-ylamino]phenols
GB Barlin, SJ Ireland, TMT Nguyen, B Kotecka and KH Rieckmann
Australian Journal of Chemistry
47(8) 1553 - 1560
Published: 1994
Abstract
Syntheses are reported for 4-(7-chloroquinolin-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 substituents have also been prepared.
In tests for antimalarial activity against the FC-27 and K-1 isolates of Plasmodium falciparum in vitro, compound (2) proved to be the most active (IC50 6.3-12.5 nM).https://doi.org/10.1071/CH9941553
© CSIRO 1994
