145431-75-0Relevant academic research and scientific papers
Potential Antimalarials. XV. Di-Mannich Bases of 2-(7'-Chloroquinolin-4'-ylamino)phenol and 2-phenol
Barlin, Gordon B.,Nguyen, Trang M. T.,Kotecka, Barbara,Rieckmann, Karl H.
, p. 1651 - 1662 (2007/10/02)
A total of 26 di-Mannich base derivatives of 2-(7'-chloroquinolin-4'-ylamino)phenol and 2-phenol, such as 2-(7'-chloroquinolin-4'-ylamino)-4,6-bis(piperidin-1"-ylmethyl)phenol, together with some 3- and 5-methyl derivatives and mono-Mannich analogues, have been prepared by condensation of the 4-chloro heterocycle with the appropriate Mannich base derivatives of 2-aminophenols.In in vitro tests against Plasmodium falciparum, many of the di-Mannich base derivatives of 2-(7'-chloroquinolin-4'-ylamino)phenolexhibited activity comparable to or superior to chloroquine against the chloroquine-sensitive (FCQ-27) isolate, and vastly superior activity compared with chloroquine against the chloroquine-resistant (K-1) isolate.Strong antimalarial activity was also revealed in in vivo tests against Plasmodium vinckei vinckei in mice.
