Antifúngicos

Applications (p-Nitrobenzylidene)malonic Acid Diethyl Ester is an potential intermediate in the preparation of fungicides that are derived from modification of Diethyl-2-benzylidenemalonate, and is potentially used for agricultural purposes.
References Sidhu, A., et al.: Pesticide. Res. J., 21, 38 (2009);

Applications N,N-Bis(4-methoxybenzyl)amine acts as a reagent for the synthesis and biological evaluation of pentanedioc acid derivatives as farnesyltransferase inhibitors. Also used in the preparation of (heteroarylamino)triazolamines as antiviral agents useful in the treatment of HCV infection.
References Yang, L., et al.: MedChemComm, 6, 671 (2015); Chen, Z., et al.: PCT Int. Appl. (2014), WO 2014135483 A1 20140912

Impurity Bifonazole EP Impurity B
Applications 5-([1,1’-Biphenyl]-4-ylphenylmethyl)-1H-Imidazole (Bifonazole EP Impurity B) is a compound derived from Bifonazole (B383400), an anti-fungal agent used in the treatment of skin diseases. Causes an increase in Ca2+ concentration and triggers cell death in PC3 human prostate cancer cells.
References Cheng, J. et al.: J. Recep. Sign. Transduct., 34, 493 (2014); Chen, Z. et al.: Mol. Pharm., 12, 590 (2015);

Sordarin sodium salt is an antifungal agent, characterized as a semisynthetic derivative produced from the fermentation products of filamentous fungi, specifically belonging to the phylum Ascomycota. This compound exerts its effects by selectively inhibiting fungal protein synthesis. It achieves this by obstructing the function of elongation factor 2 (EF-2), an essential component of fungal ribosomal activity, thereby disrupting the translational elongation step of protein synthesis.

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.

Malformin C is a cyclic pentapeptide, which is a secondary metabolite derived from certain strains of the fungus Aspergillus. Its mode of action involves disrupting cellular processes by interfering with cell division. Specifically, it is thought to affect mitotic spindle formation, leading to abnormal cell cycle progression.

21-Norrapamycin is a macrocyclic lactone antibiotic, which is derived from the bacterium Streptomyces hygroscopicus. Its chemical structure is closely related to that of rapamycin, a well-known immunosuppressant. The mode of action of 21-Norrapamycin involves the inhibition of the mechanistic target of rapamycin (mTOR) signaling pathway. By binding to the FK506-binding protein 12 (FKBP12), it forms a complex that then inhibits mTOR, a crucial regulator of cell growth, proliferation, and survival.

Beauvericin is a cyclic peptide that is isolated from the fungus Fusarium. It has been shown to have antimicrobial activity against bacteria, as well as a variety of other biological properties. Beauvericin has been shown to inhibit mitochondrial membrane potential and induce toxicity in some animal models. Beauvericin also inhibits protein synthesis and causes cell death by inhibiting DNA polymerase activity. This compound is active against cancer cells, including HL-60 cells, which are derived from human lymphocytes and are used as a model for leukemia. Beauvericin can be extracted from an ETOA extract of the fungus Fusarium oxysporum; this extract has shown anti-cancer effects in vitro assays.

Propiconazole is a triazole fungicide with action on fungal cell membranes by inhibiting ergosterol biosynthesis and is used for controlling fungal diseases in crops and turf.