Quinoline derivatives and uses thereof
AssigneeState of Oregon acting by and through the State Board of Higher Education on behalf of Portland State University
InventorsDavid H. Peyton, Steven Burgess
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Abstract
This disclosure provides a new class of compounds referred to as “reversed chloroquines” (RCQs), which are highly effective against CQR and CQS malaria parasites. RCQs are hybrid molecules, which include an antimalarial quinoline analog (such as chloroquine) moiety and a CQR reversal moiety. Exemplary RCQ chemical structures are provided. Also provided are pharmaceutical compositions including the disclosed RCQ compounds, and methods of using such compounds and compositions for the treatment of malaria and inhibition of CQR or CQS Plasmodium sp. (such as P. falciparum).
Claims6
A compound having the formula
- Q-L-G
- wherein Q represents
- wherein X1 and X2 are independently alkoxy, optionally substituted amino, halo, haloalkyl or hydroxyl;
- n is from 0 to 2;
- m is from 0 to 4;
- and R1 is H, alkyl, heteroalkyl, or alkylamino;
- wherein L is a hydrocarbon chain containing from 1 to 12 carbon atoms, optionally branched;
- and wherein G is a CQR reversal moiety having a formula selected from the structure
- wherein
- X4 is N, and R6 and R7 are independently aralkyl, heteroaryl alkyl, or heterocyclyl alkyl, or
- X4 is NHCH, R6 and R7 are aryl or heteroaryl and R6 and R7 together with X4 form a tricyclic ring system.
Dependencies are inferred from the claim text.