Tyrothricin is a polypeptide antibiotic mixture isolated from Bacillus brevis and consists of tyrocidines and gramicidins. Tyrothricin shows activity against bacteria, fungi and some viruses. Tyrothricin containing formulations are used in sore throat agents and in agents for the healing of infected superficial and small-area wounds[1].
Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle[1].
Antifungal agent 35 (compound 24) is a potent antifungal agent. Antifungal agent 35 is a potent enhancer of antifungal activity of Fluconazole against C. albicans[1].
Ketoconazole is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor.Target: CYP3A4 CYP24A1Ketoconazole, an imidazole anti-fungal agent, has often produced features of androgen deficiency including decreased libido, gynecomastia, impotence, oligospermia, and decreased testosterone levels, in men being treated for chronic mycotic infections [1]. Ketoconazole also is a cytochrome P450 inhibitor [2].Ketoconazole (KTZ), on the antischistosomal potential of these quinolines against Schistosoma mansoni infection by evaluating parasitological, histopathological, and biochemical parameters. Mice were classified into 7 groups: uninfected untreated (I), infected untreated (II), infected treated orally with PZQ (1,000 mg/kg) (III), QN (400 mg/kg) (IV), KTZ (10 mg/kg)+QN as group IV (V), HF (400 mg/kg) (VI), and KTZ (as group V)+HF (as group VI) (VII). KTZ plus QN or HF produced more inhibition (P<0.05) in hepatic CYP450 (85.7% and 83.8%) and CYT b5 (75.5% and 73.5%) activities, respectively, than in groups treated with QN or HF alone. This was accompanied with more reduction in female (89.0% and 79.3%), total worms (81.4% and 70.3%), and eggs burden (hepatic; 83.8%, 66.0% and intestinal; 68%, 64.5%), respectively, and encountering the granulomatous reaction to parasite eggs trapped in the liver.[3] CYP24A1 inhibitor enhances antiproliferative effects, increases systemic calcitriol exposure, and promotes the activation of caspase-independent apoptosis pathway.[4]
Dehydroacetic acid is an organic compound, classified as a pyrone derivative and is used mostly as a fungicide and bactericide.
Pallidol is a potent and selective singlet oxygen quencher. Pallidol shows antioxidant and antifungal activities[1][2].
Arasertaconazole is a potent 14α-lanosterol demethylase inhibitor. Arasertaconazole has antifungal and antibacterial activity[1].
Antibacterial agent 73 (compound 7a) is a potent antimicrobial agent. Antibacterial agent 73 exhibits very good antitubercular activity (MIC=0.65 µg/mL) against Mtb H37Rv. Antibacterial agent 73 shows good activity against fungal and bacterial. Antibacterial agent 73 also shows cytotoxicity in MCF-7 breast cancer cell lines, with IC50 of 8.20 μM[1].
5-(Hydroxymethyl)furan-2-carbaldehyde, derived from lignocellulosic biomass, inhibits yeast growth and fermentation as stressors.
PD 113270 (CL 1565-B) is an antitumor agent. PD 113270 exhibits inhibitory effects to yeasts[1].
Swinholide A is the actin-binding marine polyketide and dimerizes actin with the Kd of ~ 50 nM[1]. Swinholide A is a microfilament disrupting marine toxin that stabilizes actin dimers and severs actin filaments. Swinholide A disrupts the actin cytoskeleton of cells.Antifungal activity[2].
Neophellamuretin is a flavonoid. Neophellamuretin inhibits Trichophyton sp. with an MIC value of 62.5 µg/mL[1].
Inz-5 is a fungal-selective mitochondrial cytochrome bc1 inhibitor. Inz-5 impairs fungal virulence and prevents the evolution of drug resistance[1].
Rhamnolipid RL2, is a rhamnolipid, shows antifungal activity[1][2].
Metalaxyl-M ((R)-Metalaxyl) is the active (R)-enantiomer of Metalaxyl. Metalaxyl-M is a broad-spectrum fungicide that inhibits protein and ribosomal RNA synthesis in fungi. Metalaxyl is used for research of plant diseases caused by pathogens of the Oomycota division[1].
4-Isopropylbenzoic acid, an aromatic monoterpenoid, is isolated from the stem bark of Bridelia retusa. 4-Isopropylbenzoic acid exhibits antifungal activities. 4-Isopropylbenzoic acid is also a reversible and uncompetitive inhibitor of mushroom tyrosinase[1][2].
Butoconazole nitrate is an anti-fungal agent.Target: Antifungalbutoconazole 1-BSR is an effective and safe alternative to longer-term therapy with miconazole nitrate (seven days) for vulvovaginal candidiasis [1]. A sustained-release (SR) bioadhesive vaginal cream (2% butoconazole nitrate) has incorporated VagiSite technology, a topical drug delivery system that allows SR of the drug [2].
3,5-Di-tert-butylphenol is an volatile organic compound with anti-biofilm and antifungal activities. 3,5-Di-tert-butylphenol induces accumulation of reactive oxygen species (ROS).
Fenpropimorph is a fungicide that inhibits the sterol pathway. Fenpropimorph inhibits δ8-δ7-sterol isomerase in yeast at low concentrations, with δ14-sterol reductase being blocked at higher levels, preventing the biosynthesis of ergosterol. Fenpropimorph also inhibits sterol synthesis in certain plants and mammalian cells[1][2][3].
Fungicide4 shows the high activity against the P. infestans strain.
10-Undecenoic acid zinc salt is a natural or synthetic fungistatic fatty acid, is used topically in creams against fungal infections, eczemas, ringworm, and other cutaneous conditions. The zinc provides an astringent action.
SMAP-29, a promising antiinfective agent, is a broad spectrum antibacterial and antifungal α-helical cathelicidin-derived peptide. SMAP-29 acts by permeabilizing bacterial membranes and inducing remarkable changes in the surface morphology of susceptible microorganism[1][2].
Propiconazole is a broad-spectrum triazole fungicide that inhibits the conversion of lanosterol to ergosterol, leading to fungal cell membrane disruption. Propiconazole inhibits S. cerevisiae, but not rat liver, microsomal cytochrome P450 (IC50s = 0.04 µM and >200 µM, respectively). Propiconazole inhibits the growth of T. deformans and R. stolonifer (ED50s = 0.073 µg/mL and 4.6 µg/mL respectively). Propiconazole increases production of reactive oxygen species (ROS).
Fluazinam impurity 1 is an impurity of Fluazinam with antifungal activity. Fluazinam impurity 1 is active against Sphaerotheca fuliginea, Pyricularia oryzae and Rhizoctonia solani[1].
Viridicatol, a quinolinone alkaloid, is isolated from the fermentation of an endophytic fungus Penicillium sp. R22 in Nerium indicum. Viridicatol has strong antifungal activity against Staphylococcus aureus with MIC value of 15.6 μg/mL[1].
Butenafine hydrochloride is a synthetic benzylamine antifungal, works by inhibiting the synthesis of sterols by inhibiting squalene epoxidase.IC50 Value: Target: Antifungal; squalene epoxidaseButenafine Hydrochloride, a benzylamine derivative, is an antifungal which is used to control dermal fungal infections such as athletes foot and ring worm. Butenafine Hydrochloride is squalene epoxidase inhibitor, inhibits the synthesis of ergosterol needed in fungal cell membranes. The drug has excellent penetration into the epidermis and a prolonged retention time following topical application, conferring residual therapeutic activity after treatment cessation. Butenafine possess anti-inflammatory activity too. Butenafine hydrochloride 1% cream is safe and effective for tinea corporis cruris and tinea manuum pedis.
Neticonazole hydrochloride is an imidazole derivative and a potent and long-acting antifungal agent. Neticonazole hydrochloride is also an orally active exosome biogenesis and secretion inhibitor. Neticonazole hydrochloride has anti-infection and anti-cancer effects[1][2][3].
Moracin D is a flavonoid that can be isolated from Morus alba. Moracin D induces cell apoptosis and shows hypoglycemic, antiadipogenic, antifungal and antitumor effects. Moracin D can be used for fungal infection and breast cancer research[1][2][3].
PC945 is a novel broad spectrum antifungal agent that potently inhibits Aspergillus fumigatus sterol 14α-demethylase (CYP51A and CYP51B) with IC50 of 0.23 and 0.22 uM, respectively; shows MIC values 0.032 to >8 ug/ml against 96 clinically isolated A. fumigatus strains, demonstrates activity against itraconazole-susceptible and -resistant A. fumigatus growth with IC50 of 0.0012 to 0.034 ug/ml; PC945 is a broad spectrum of pathogenic fungi with MIC 0.0078 to 2 ug/ml, and exhibits activity in vivo. Fungal Infection Phase 1 Clinical