Imidazopyridine · Lablypedia

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Sedatives

Anxiolytics, sedatives and hypnotics (GABA_A receptor positive allosteric modulators):

Imidazo[1,2-a]pyridines:
- Alpidem (original brand name Ananxyl)—an anxiolytic that was withdrawn from the market worldwide in 1995 due to hepatotoxicity.
- DS-1—a GABA_A receptor positive allosteric modulator selective for the α₄β₃δ subtype, which is not targeted by other GABAergics such as benzodiazepines or other nonbenzodiazepines.
- Necopidem—an anxiolytic. It has not found clinical use.
- Saripidem—a sedative and anxiolytic. It is not used clinically.
- TP-003—a subtype-selective partial agonist at GABA_A receptors, binding to GABA_A receptor complexes bearing either α₂, α₃ or α₅ subunits, but only showing significant efficacy at α₃.
- Zolpidem (original brand name Ambien)—a widely used hypnotic. Generic versions are widely available.
Imidazo[4,5-c]pyridines:
- Bamaluzole—a GABA_A receptor-agonizing anticonvulsant that was never marketed.

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Imidazo[1,2-a]pyridines:
- Mosapramine (brand name クレミン, Cremin)—an atypical antipsychotic used in Japan.

Drugs used for peptic ulcer disease (PUD), GERD and gastroprokinetic agents (motility stimulants):

Imidazo[1,2-a]pyridines:
- CJ-033466—an experimental gastroprokinetic acting as a selective 5-HT₄ serotonin receptor partial agonist.
- Zolimidine—a gastroprotective agent.
- Linaprazan—a potassium-competitive acid blocker which demonstrated similar efficacy as esomeprazole in healing and controlling symptoms of GERD patients with erosive esophagitis.
- SCH28080—the prototypical potassium-competitive acid blocker which has not found clinical use because of liver toxicity in animal trials and elevated liver enzyme activity in the serum of human volunteers.
Imidazo[4,5-b]pyridines:
- Tenatoprazole—it blocks the gastric proton pump leading to decline of gastric acid production.

NSAIDs, analgesics and antimigraine drugs:

Imidazo[1,2-a]pyridines:
- Miroprofen—a derivative of propionic acid.
Imidazo[4,5-b]pyridines:
- Telcagepant—a calcitonin gene-related peptide receptor antagonist which was in clinical trials as a remedy for migraine. Its development was terminated.

Drugs for treatment of bone diseases:

Imidazo[1,2-a]pyridines:
- Minodronic acid (brand names Bonoteo, Recalbon)—a third-generation bisphosphonate used for the treatment of osteoporosis.

Antineoplastic agents:

Imidazo[1,5-a]pyridines:
- Fadrozole (brand name Afema)—an aromatase inhibitor.
Imidazo[4,5-c]pyridines:
- 3-Deazaneplanocin A—an S-adenosyl-L-homocysteine synthesis inhibitor and histone methyltransferase EZH2 inhibitor.

Directly-acting antiviral agents:

Imidazo[1,2-a]pyridines:
- Tegobuvir (GS-9190) - an allosteric, non-nucleoside hepatitis C virus NS5B RNA-dependent RNA polymerase inhibitor targeting the thumb II allosteric site.