Diarylquinolines (DARQs) is a chemical class of drugs that treat tuberculosis, They target subunit c of mycobacterial ATP synthase, inhibiting the enzyme so mycobacterium tuberculosis cannot synthesise ATP. This effectively kills the bacteria.
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Although ATP synthase in bacteria is similar to its eukaryotic analogue, diarylquinoline agents (such as TMC207) are very specific to the bacterial enzyme, so were expected to be safe for use in humans and other eukaryotes. This also suggests that bacterial ATP synthase inhibition is an attractive therapeutic target
Examples
Synthesis of 1,4-diarylquinolines
The reaction of arylaldehyde, malonodinitrile, and 3‐arylamino‐5,5‐dimethylcyclohex‐2‐enone can produce 1,4-diarylquinolines.
Synthesis of 2,4-diarylquinolines
The reaction of enamides and imines can produce heteroaromatic quinoline derivatives.