Antifungals

1-Isomangostin hydrate, a natural product extracted from the Mangosteen vine, exhibits antifungal activity.

Butoconazole nitrate is an antifungal agent and is used for the treatment of vaginal yeast infections. It inhibits the synthesis of ergosterol, disrupting the fungal cell membrane.

Pafuramidine is an antiprotozoal prodrug with action on protozoal DNA synthesis inhibition and is used for treating African sleeping sickness and Pneumocystis pneumonia.

Sulbentine (Dibenzthione) is an antifungal agent.

Benodanil (Calirus) is a kind of fungicide.

Abafungin is an antifungal agent and is used for treating fungal infections.

Applications An isotopically Labelled metabolite of Itraconazole, an orally active antimycotic structurally related to Ketoconazole. It is a COVID19-related research product. References Saag, M., et al.: Antimicrob. Agents Chemother., 32, 1 (1988), Haria, M., et al.: Drugs, 51, 585 (1996), Kousoulos, C., et al.: Anal. Bioanal. Chem., 384,199 (2006),

Triclopyr (NSC 190671) is a synthetic growth hormone-like herbicide and fungicide with cytotoxicity and mitochondrial damage induced in rat liver

Applications Deoxo Anhydro Itraconazole Bromide is an impurity of Itraconazole (I937500), which is orally active antimycotic drug structurally related to Ketoconazole (K186000). Antifungal. It is a COVID19-related research product. References Espinel-Ingroff, A., et al.: Antimicrob. Agents Chemother., 26, 5 (1984); Heykants, J., et al.: Mycoses, 32, Suppl 1, 67 (1989); Sugar, A.M.,et al.: Curr. Clin. Top. Infect. Dis., 13, 74 (1993);

Fengycin A analogue is an antifungal lipopeptide, which is a cyclic compound derived from microbial sources, specifically produced by Bacillus subtilis strains. It functions primarily by disrupting the cell membranes of pathogenic fungi, leading to altered membrane permeability and subsequent cell death. The unique structure of fengycin allows it to interact with membrane lipids, compromising membrane integrity and inhibiting fungal growth. The uses and applications of Fengycin A analogue are notable in agricultural settings, where it serves as a biocontrol agent against various fungal pathogens affecting crops. Its role extends to contributing to sustainable agricultural practices by reducing the need for chemical fungicides. Additionally, it is of interest in pharmaceutical research due to its potential therapeutic applications against fungal infections. The compound's specific mode of action and natural origin make it a promising candidate for further investigation in both the development of novel antifungal strategies and the enhancement of plant health.

Eberconazole Nitrate (Ebernet) is an azole antifungal agent and broad-spectrum imidazole derivative.

Kanosamine (3-Amino-3-deoxyglucose) is an antifungal agent produced by a Streptomyces sp.

Phenylethyl isothiocyanate (JC5411) is an HDAC inhibitor. It potentially for the treatment of benign prostatic hypertrophy.

Picropodophyllone is one of the lignans from the roots of D. aurantiocaulis and D. pleianthum.

Applications 2-[[[1-(4-Chlorophenyl)-1H-pyrazol-3-yl]oxy]methyl]benzenamine is an intermediate used in the synthesis of (P840402), which is an isotope labelled Pyraclostrobin, a fungicide for use in seed grass and food crops. References Gyldenkaerne, S., et al.: Pestic Sci., 55, 1210 (1999), Pennington, D., et al.: Environ. Sci. Technol., 39, 1119 (2005), Wang, S., et al.: Food Control., 18, 731 (2007),

Fosravuconazole L-lysine ethanolate, a prodrug for ravuconazole, treats onychomycosis in Japan.

Embeconazole (R 120758) is a triazole antifungal agent with strong in vitro activity against clinically important fungi such as Candida and Aspergillus.

Quinoxyfen has antimicrobial activity and can be used to study powdery mildew.

FBA-IN-1 (2a11) is the first covalent, allosteric CaFBA inhibitor, effective against Azole-resistant strains with a MIC 80 of 1 μg/mL.

Aureothin is a bioactive compound, classified as a polyketide antibiotic, which is derived from the culture of the bacterium Streptomyces thioluteus. This compound operates primarily through the inhibition of protein synthesis by interfering with the aminoacylation of tRNA with specific amino acids. Its mode of action disrupts cellular protein synthesis, which is essential for cell growth and function, leading to its potent antibacterial and antifungal activities. Aureothin exhibits a broad spectrum of uses and applications. In microbiological and pharmaceutical research, it serves as an important tool for studying microbial resistance mechanisms and protein synthesis pathways. Its application extends to agricultural research, where it is evaluated for controlling pathogenic fungi and invasive plant species due to its herbicidal properties. The compound’s dual action as both an antimicrobial and herbicidal agent makes it valuable in the development of new agrochemicals and therapeutic strategies against infections. Scientists continue to explore its biosynthesis and potential modifications to enhance its efficacy and specificity.

NB-598 is an effective and competitive inhibitor of squalene epoxidase. It suppresses triglyceride biosynthesis through the farnesol pathway.

Metalaxyl (CGA 48988) is a fungicide that inhibits protein synthesis in fungi and interferes with skeletal development in zebrafish embryos.

Fenhexamid (Elevate), a sterol biosynthesis inhibitor, shows antifungal activity against the plant pathogenic fungus.

Filipin III is a polyene macrolide antibiotic, which is extracted from Streptomyces filipinensis. Known for its unique mode of action, Filipin III interferes with cholesterol-rich membranes by binding to ergosterol and cholesterol. This interaction disrupts the membrane structure, altering membrane permeability and ultimately affecting cell viability. In scientific research, Filipin III is utilized predominantly as a biochemical probe to detect and study cholesterol distribution within cell membranes. Its affinity for sterol structures makes it invaluable for understanding cholesterol dynamics and membrane organization in eukaryotic cells. By exploiting its membrane-disturbing properties, researchers can elucidate cellular processes involving sterol-rich domains and their roles in various physiological functions. Additionally, its antifungal properties offer a basis for studying membrane integrity-related pathogen resistance mechanisms, though its clinical application is limited due to cytotoxicity. This agent allows for profound insights into the molecular composition and behavior of cellular membranes, serving as a tool in the toolkit of cell and molecular biologists.

Caerulomycin A (Caerulomycin) (Cerulomycin; Caerulomycin) is an antifungal compound.

Ethyl 4-bromocrotonate ((E)-Ethyl 4-bromobut-2-enoate) is an antimicrobial compound belonging to the ester group. As an important pharmaceutical intermediate, it has been used as a substrate for enzyme-catalyzed reactions, and as a tool for studying enzyme kinetics. It has also been found to have anti-inflammatory and analgesic properties.

Itraconazole (R51211) is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis.

Paclobutrazol ((R,R)-paclobutrazol) is a triazole-containing plant growth retardant that is known to inhibit the biosynthesis of gibberellins.1,2It also has

Broad spectrum imidazole antifungal

Applications TH-302 is a 2-nitroimidazole triggered hypoxia-activated prodrug (HAP) of bromo-isophosphoramide mustard. Studies have shown that TH-302 treatment exhibited hypoxia-selective cytotoxicity and DNA damage in human cancer cell References Meng, F. et al.: Mol. Cancer Ther., 11, 740 (2012); Liu, Q. et al.: Cancer Chemother. Pharmacol., 69, 1487 (2012); Sun, J.D. et al.: Clin. Cancer Res., 18, 758 (2012);

Applications A bactericidal and fungicidal. References Schoppelrei, J., et al.: J. Phys. Chem., 100, 14343 (1996), Kolb, H., et al.: Drug Discovery Today, 8, 1128 (2003),

Nikkomycin Z (Nikkomycin Z from Streptomyces tendae) is a competitive chitin synthase inhibitor.It inhibitor of the growth of filamentous fungi, insects,

Loflucarban (Fluonilid) is an antimycotic compoud.

FR194738 is an inhibitor of squalene epoxidase with an IC50 of 9.8 nM in HepG2 cell homogenates.

Applications Gliotoxin is a sulfur-containing mycotoxin produced by species of fungi and pathogens of humans. Gliotoxin exhibits inhibitory activities against histone H3K9 methyltransferase, a key enzyme in the regulation of transcriptional activity by writing epigenetic marks. Gliotoxin also exhibits immunosuppressive properties by causing apoptosis of cells of the immune system. In addition, various studies suggests Gliotoxin may also be a potential anti-inflammatory, antibiotic, antifungal and antiviral agent. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Takahashi, M., et al.: J. Antibiotics., 65, 263 (2012); Li., Y.G., et al.: Biochem. Biophy. Rsch. Commun., 422, 85 (2012); Zhang, H.C., et al.: Applied, Mech. Mater., 178, 783 (2012); Scharf, D.H., et al.: Appl. Microbiol. Biotechnol., 93, 467 (2012);

Ceftriaxone: cephalosporin antibiotic, effective against Gram-positive/negative bacteria, with anti-inflammatory/antioxidant properties.

Neoaureothin is a natural antibiotic product, which is derived from marine actinomycetes with a complex polyketide structure. Its mode of action involves the inhibition of bacterial protein synthesis by binding selectively to the ribosomal subunits, thereby obstructing the translation process in susceptible microbial strains. The specificity of its action allows it to target a broad spectrum of Gram-positive bacteria while presenting a lower risk of resistance development compared to traditional antibiotics. Neoaureothin is utilized extensively in research settings to explore novel antibacterial pathways and potential therapeutic applications in combating resistant bacterial strains. Its unique source and mode of action make it a valuable tool in the study of marine-derived antibiotics, offering insights into alternative treatment strategies for bacterial infections. Researchers often employ this compound in experimental assays to gauge inhibition potency, elucidate biological pathways, and refine synthetic analogues for enhanced efficacy.

Pan-histone demethylase inhibitor; anti-fungal; iron-chelator

Applications Labelled Isavuconazole (I777832). It is a new triazole currently undergoing phase III clinical trials. This compound has shown in vitro activity against a large number of clinical important yeasts and molds including Aspergillus spp., Fusarium spp., Scedosporium spp., Candida spp., the Zygomycetes and Cryptococcus spp. References Ohwada, J., et al.: Bioorg. Med. Chem. Lett., 13, 191 (2003), Guinea, J., et al.: Antimicrob. Agents Chemother., 52, 1396 (2008)