Diarylquinoline

Diarylquinoline is a class of antibacterial drugs that are primarily used in the treatment of tuberculosis. The most notable drug in this class is Bedaquiline, which was approved by the Food and Drug Administration (FDA) in 2012 for the treatment of multi-drug resistant tuberculosis (MDR-TB).

History

The discovery of diarylquinoline as an effective antitubercular agent was a significant breakthrough in the field of pharmacology. The first diarylquinoline, Bedaquiline, was developed by Janssen Pharmaceutica, a division of Johnson & Johnson. It was the first new class of drugs approved for the treatment of tuberculosis in over 40 years.

Mechanism of Action

Diarylquinolines work by inhibiting the ATP synthase of Mycobacterium tuberculosis, the bacterium that causes tuberculosis. This inhibition disrupts the bacterium's energy metabolism, leading to cell death. This mechanism of action is unique among antitubercular drugs, making diarylquinolines a valuable tool in the fight against drug-resistant strains of tuberculosis.

Clinical Use

Diarylquinolines are used in the treatment of MDR-TB, a form of tuberculosis that is resistant to at least two of the main first-line drugs, isoniazid and rifampicin. They are typically used in combination with other antitubercular drugs to prevent the development of further drug resistance.

Side Effects

Like all drugs, diarylquinolines can have side effects. The most common side effects include nausea, joint pain, and headache. More serious side effects can include liver damage and an irregular heartbeat. Because of these potential side effects, diarylquinolines are typically reserved for cases where other treatments have failed.

Future Research

Research is ongoing into the potential uses of diarylquinolines in the treatment of other diseases caused by mycobacteria, such as leprosy and Buruli ulcer. There is also interest in developing new drugs in the diarylquinoline class that may be more effective or have fewer side effects.