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| Other names | O-(1,2,3,4-Tetrahydro-1,4-methanonaphthalen-6-yl) m,N-dimethylthiocarbanilate [1] |
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| ECHA InfoCard | 100.051.611 |
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| Formula | C20H21NOS |
| Molar mass | 323.45 g·mol−1 |
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Tolciclate (INN) [1] : 9 is an antifungal medication. [2] [3]
Tolnaftate (INN) is a synthetic thiocarbamate used as an anti-fungal agent that may be sold without medical prescription in most jurisdictions. It is supplied as a cream, powder, spray, liquid, and liquid aerosol. Tolnaftate is used to treat fungal conditions such as jock itch, athlete's foot and ringworm.
Anidulafungin (INN) is a semisynthetic echinocandin used as an antifungal drug. It was previously known as LY303366. It may also have application in treating invasive Aspergillus infection when used in combination with voriconazole. It is a member of the class of antifungal drugs known as the echinocandins; its mechanism of action is by inhibition of (1→3)-β-D-glucan synthase, an enzyme important to the synthesis of the fungal cell wall.
Clorgiline (INN), or clorgyline (BAN), is a monoamine oxidase inhibitor (MAOI) structurally related to pargyline which is described as an antidepressant. Specifically, it is an irreversible and selective inhibitor of monoamine oxidase A (MAO-A). Clorgiline was never marketed, but it has found use in scientific research. It has been found to bind with high affinity to the σ1 receptor (Ki = 3.2 nM) and with very high affinity to the I2 imidazoline receptor (Ki = 40 pM).
Urtoxazumab is a humanized monoclonal antibody against diarrhoea caused by Escherichia coli, serotype O121. The drug is designed to bind to a toxin of this bacterium, so that it can be more easily broken down and eliminated from the body.
Fleroxacin is a quinolone antibiotic. It is sold under the brand names Quinodis and Megalocin.
Carumonam (INN) is a monobactam antibiotic. It is very resistant to beta-lactamases, which means that it is more difficult for bacteria to break down using β-lactamase enzymes.
Ravuconazole is a potent triazole antifungal, the development of which was discontinued in 2007. The drug has shown to have a similar spectrum of activity to voriconazole, with an increased half-life. However, ravuconazole has limited activity against species of Fusarium, Scedosporium, and Zygomycetes.
Albaconazole is an experimental triazole antifungal. It has potential broad-spectrum activity. The drug blocks a number of CYP450 liver enzymes.
Aminocandin is an echinocandin antifungal. It works by targeting the glucan in fungal cell walls.
Censavudine (INN) (BMS-986001) is an investigational new drug being developed by Bristol Myers-Squibb for the treatment of HIV infection. It was originally developed at Yale University.
Gepotidacin (INN) is an experimental antibiotic that acts as a topoisomerase type II inhibitor. It is being studied for the treatment of uncomplicated urinary tract infection and infection with Neisseria gonorrhoeae (gonorrhea), including multidrug resistant strains.
Vaborbactam (INN) is a non-β-lactam β-lactamase inhibitor discovered by Rempex Pharmaceuticals, a subsidiary of The Medicines Company. While not effective as an antibiotic by itself, it restores potency to existing antibiotics by inhibiting the β-lactamase enzymes that would otherwise degrade them. When combined with an appropriate antibiotic it can be used for the treatment of gram-negative bacterial infections.
Danoprevir (INN) is an orally available 15-membered macrocyclic peptidomimetic inhibitor of NS3/4A HCV protease. It contains acylsulfonamide, fluoroisoindole and tert-butyl carbamate moieties. Danoprevir is a clinical candidate based on its favorable potency profile against multiple HCV genotypes 1–6 and key mutants (GT1b, IC50 = 0.2–0.4 nM; replicon GT1b, EC50 = 1.6 nM). Danoprevir has been evaluated in an open-label, single arm clinical trial in combination with ritonavir for treating COVID-19 and favourably compared to lopinavir/ritonavir in a second trial.
Glecaprevir (INN,) is a hepatitis C virus (HCV) nonstructural (NS) protein 3/4A protease inhibitor that was identified jointly by AbbVie and Enanta Pharmaceuticals. It is being developed as a treatment of chronic hepatitis C infection in co-formulation with an HCV NS5A inhibitor pibrentasvir. Together they demonstrated potent antiviral activity against major HCV genotypes and high barriers to resistance in vitro.
Orotomides are a class of experimental antifungals. They were discovered in 2015 by British scientists at the pharmaceutical company F2G Ltd. while searching for a new drug for Aspergillus infection. The discovery was formally announced at the Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) 55th meeting during 17-21 September 2015 at San Diego, California, and published the next year in the Proceedings of the National Academy of Sciences. It was found to be effective against most important human fungal infections including those with Aspergillus, Lemontospora (Scedosporium) prolificans, Fusarium, Penicillium spp., and Taloromyces. The most promising drug candidate is designated F901318, chemical name 2-(1,5-dimethyl-3-phenyl-1H-pyrrol-2-yl)-N-{4-[4-(5-fluoro-pyrimidin-2-yl)piperazin-1-yl]-phenyl}-2-oxo-acetamide. F901318 has been named Olorofim.
Karen Bush is an American biochemist. She is a Professor of Practice in Biology at Indiana University and the interim director of the Biotechnology program. Bush conducts research focusing on bacterial resistance mechanisms to beta-lactam antibiotics.
4α-Methylfecosterol is a metabolic intermediate of sterols made by certain fungis, can be converted to 24-Methylenelophenol by enzyme HYD1, or undergo 4-demethylation to fecosterol.
Karen Joy Shaw is an American microbiologist and discoverer of novel antifungal and antibacterial compounds. She is best known for her work on aminoglycoside resistance in bacteria as well as leading drug discovery research teams. As Senior Vice President of Biology at Trius Therapeutics, Inc. her work was critical to the development of the oxazolidinone antibiotic tedizolid phosphate (Sivextro) as well as the discovery of the TriBE inhibitors, a novel class of DNA gyrase/Topoisomerase IV antibacterial agents that target both Gram-positive and Gram-negative organisms.[2] As Chief Scientific Officer at Amplyx Pharmaceuticals, Shaw was responsible for the preclinical development of the novel antifungal fosmanogepix, a first-in-class broad-spectrum antifungal prodrug that is currently in Phase 2 clinical development for the treatment of invasive fungal infections. She also discovered APX2039, a unique Gwt1 inhibitor that is in preclinical development for the treatment of cryptococcal meningitis.
Sulopenem (CP-70,429) is an antibiotic derivative from the carbapenem family, which unlike most related drugs is orally active. It was developed in Japan in the 1990s but has never been approved for medical use, however it has reached Phase III clinical trials on several occasions and continues to be the subject of ongoing research into potential applications, especially in the treatment of multiple drug resistant urinary tract infections.
Fosmanogepix is an experimental antifungal drug being developed by Pfizer. It is being investigated for its potential to treat various fungal infections including aspergillosis, candidaemia, and coccidioidomycosis.
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