Imidazoles

Imetit is a histamine H3 receptor agonist.

Proxyfan is a histamine H3 receptor ligand which is a "protean agonist", producing different effects ranging from full agonist, to antagonist, to inverse agonist in different tissues, depending on the level of constitutive activity of the histamine H3 receptor. This gives it a complex activity profile in vivo which has proven useful for scientific research.

α-Methylhistamine is a synthetic derivative and a selective histamine H3 receptor agonist. It decreases blood pressure and heart rate in guinea pigs. The drug also has sedative and hypnotic effects in animals.

Cipralisant (GT-2331, tentative trade name Perceptin) is an extremely potent histamine H3 receptor ligand originally developed by Gliatech. Cipralisant was initially classified as a selective H3 antagonist, but newer research (2005) suggests also agonist properties, i.e., functional selectivity.

Acadesine (INN), also known as 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside, AICA-riboside, and AICAR, is an AMP-activated protein kinase activator which is used for the treatment of acute lymphoblastic leukemia and may have applications in treating other disorders such as diabetes. Acadesine has been used clinically to treat and protect against cardiac ischemic injury. The drug was first used in the 1980s as a method to preserve blood flow to the heart during surgery.

Oxmetidine (development code SKF 92994) is an H2 histamine receptor receptor antagonist.

Lophine is the organic compound with the formula . It is a derivative of imidazole wherein all three carbon atoms have phenyl groups as substituents. A white solid, this compound gave the first example of chemiluminescence when its basic solutions were exposed to air. Its chemiluminescence continues to attract attention.

Immethridine (developmental code name BP-1-5375) is a histamine agonist selective for the H3 subtype.

Ozagrel (INN) is an antiplatelet agent working as a thromboxane A2 synthesis inhibitor. ==Synthesis== upright=2 The free-radical halogenation of ethyl 4-methylcinnamate (1) with N-bromosuccinimide in the presence of benzoyl peroxide gives ethyl 4-bromomethylcinnamate (2). Alkylation of imidazole (3) with this material gives the ethyl ester (4) of the drug, which is saponified to give ozagrel.

Ciproxifan is an extremely potent histamine H3 inverse agonist/antagonist.

Ethonam is an antifungal agent.

Nafimidone is an anticonvulsant drug of the imidazole class. It contains a naphthyl group. It seems to have been discovered by accident during a search for antifungal agents.

Prochloraz, brand name Sportak, is an imidazole fungicide that was introduced in 1978 and is widely used in Europe, Australia, Asia, and South America within gardening and agriculture to control the growth of fungi. It is not registered for use in the United States.

Clobenpropit is a histamine H3 receptor antagonist. It has neuroprotective effects via stimulation of GABA release in brain cells in vitro.

Mizoribine (INN; MZB; trade name Bredinin) is an immunosuppressive drug. The compound was first observed in Tokyo, Japan, in 1971. It was first isolated from the fungus Penicillium brefeldianum. Mizoribine is an imidazole nucleoside that has been used in renal transplantation, and in steroid-resistant nephrotic syndrome, IgA nephropathy, lupus, as well as for adults with rheumatoid arthritis, lupus nephritis and other rheumatic diseases. MZB exerts its activity through selective inhibition of inosine monophosphate dehydrogenase and guanosine monophosphate synthetase, resulting in the complete

Tipifarnib (INN, proposed trade name Zarnestra) is a farnesyltransferase inhibitor. Farnesyltransferase inhibitors block the activity of the farnesyltransferase enzyme by inhibiting prenylation of the CAAX tail motif, which ultimately prevents Ras from binding to the membrane, rendering it inactive.