Lyoniside is a lignan glycoside with antioxidant, allelopathic and antifungal activities, which can be isolated from the rhizomes and stems of bilberry (Vaccinium myrtillus L.). Lyoniside exhibits radical scavenging properties with an IC50 value of 23 μg/mL in DPPH assay. Lyoniside inhibits the mycelial growth of Fusarium oxysporum and Mucor hiemalis at 50 μg/mL with inhibitory rates of 78% and 80%, respectively[1].
L18-MDP is a derivative of muramyl dipeptide, an antibacterial agent. L18-MDP has antibacterial activity and has potential applications in bacterial and fungal infections[1].
Diallyl Trisulfide is isolated from Garlic. Diallyl Trisulfide suppresses the growth of Penicillium expansum (MFC99 value: ≤ 90 μg/mL) and promotes apoptosis via production of reactive oxygen species (ROS) and disintegration of cellular ultrastructure. Anticancer effect[1].
Fosmanogepix (APX001) is a first-in-class and orally available broad-spectrum antifungal agent, which targets the highly conserved Gwt1 fungal enzyme. Fosmanogepix (APX001) is an N-phosphonooxymethyl prodrug which is rapidly and completely metabolized by systemic alkaline phosphatases to the active moiety, APX001A. Fosmanogepix (APX001) can be used in development for the treatment of invasive fungal infections[1][2].
Y18501 is a oxysterol-binding protein (OSBPI) inhibitor with a similar structure to Oxathiapiprolin. Y18501 shows strong inhibitory activities against Phytophthora spp. and Pseudoperonospora cubensis, with EC50 ranging from 0.0005 to 0.0046 μg/mL. Y18501 shows excellent protective and curative activities against P. cubensis. Y18501 in combination with Chlorothalonil (HY-N6625) can significantly promote the inhibition of P. cubensis[1].
Fluconazole (hydrate) is a triazole antifungal drug used in the treatment and prevention of superficial and systemic fungal infections.Target: AntifungalFluconazole (hydrate) is the hydrate salt form of fluconazole, which is a triazole antifungal intended for oral treatment of superficial and systemic mycoses. In tests done in standard mycological media, the compound had minimal inhibitory concentrations against pathogenic Candida species that were usually in excess of 100 mg/l. Fluconazole inhibited branching and hyphal development in C. albicans at concentrations as low as 10(-6) M (0.3 mg/l), but miconazole and ketoconazole were still active in these tests at concentrations 100 times lower than this [1]. Oral fluconazole was not associated with a significantly increased risk of birth defects overall or of 14 of the 15 specific birth defects of previous concern. Fluconazole exposure may confer an increased risk of tetralogy of Fallot [2]. Fluconazole is predicted to be ineffective against Cryptococcus gattii in the koala as a sole therapeutic agent administered at 10 mg/kg p.o. every 12 h [3].Clinical indications: Balanitis; Candida infection; Cryptococcus infection; Cryptococcus neoformans meningitis; Dermatomycosis; Female genital tract infection; Fungal infection; Fungal respiratory tract infection; Fungal urinary tract infection; Prophylaxis; Tinea capitis; Tinea corporis; Tinea cruris; Tinea pedis .Toxicity: Symptoms of overdose include hallucinations and paranoid behavior.
Canadensolide is an antifungal metabolite of Penicillium canadense.
Diamthazole (Dimazole) hydrochloride is an antifungal agent. Diamthazole hydrochloride can be used for the research of infection[1].
Griseofulvin-13C,d3 is the 13C- and deuterium labeled.
3α,22β-Dihydroxyolean-12-en-29-oic acid is a terpenoid isolated from Maytenus royleanus cufodontis. 3α,22β-Dihydroxyolean-12-en-29-oic acid shows antiproliferative activity for HeLa, PC-3 and HCCLM3 cell lines with an IC50 values of 32.64 µM, 9.09 µM and 6.9 µM, respectively[1][2][3].
Gliovirin is an antibiotic active against Pythium ultimum. Gliovirin is isolated from Gliocla-dium virens. Gliovirin may be derived from L,L-phenylalanine anhydride, which is also isolated from G. virens[1].
L-Diguluronic acid is a linear polysaccharide copolymer composed of two L-guluronic acid (G) and can be used to from Alginate[1]. Alginate is a generic name of unbranched polyanionic polysaccharides and can be used for the research of antifungal agents delivery carries[2].
Melittin free acid is a basic 26-amino-acid polypeptide, the major active ingredient of honeybee venom. Melittin free acid is an activator of phospholipase A2 (PLA2). Melittin free acid has broad-spectrum antifungal activity with MIC values of 0.4-60 μM. Melittin free acid hinders fungal growth by inducing cell apoptosis, repressing (1,3)-β-D-glucan synthase and participating in other pathways[1][2].
Sertaconazole nitrate is a topical broad-spectrum antifungal that is developed to provide an additional agent for the treatment of superficial cutaneous and mucosal infections.Target: AntifungalSertaconazole nitrate reduces the release of cytokines from activated lymphocytes and mitigated inflammation in animal models of irritant contact dermatitis and neurogenic inflammation in a dose-dependent fashion. Sertaconazole nitrate is found to inhibit the proliferation of stimulated human lymphocytes with IC50 of 4 μg/mL [1]. Sertaconazole nitrate inhibits ergosterol synthesis by blockade of the P450-dependent enzyme pathway that catalyzes the methylation of lanosterol to ergosterol, thus inhibits fungal cell growth. Sertaconazole nitrate binds directly to nonsterol lipids in the membrane, which interferes with the regulation of the permeability of fungal cell membranes, thus induces fungal cell death [2].The mean ear weight of Tetradecanoyl phorbol acetate (TPA)-challenged murine treated with sertaconazole nitrate (1%) is 7.23 mg compared with 14.7 mg for controls, indicating a statistically significant reduction in irritant dermatitis. Sertaconazole nitrate 1% elicits a significant reduction in Resiniferatoxin-induced ear edema when compared with controls in CD-1 mice. Topical treatment with sertaconazole nitrate 1% significantly inhibits contact hypersensitivity and decreases the content of the pro-inflammatory cytokines TNFα, IL-2, and IFNγ in oxazolone exposed murine skin [1]. Clinical trials with sertaconazole nitrate cream 2% show efficacy in the treatment of superficial cutaneous fungal infections [2]. Sertaconazole reduces inflammation via inducing PGE2 production and the COX-2 inhibitor blocks sertaconazole from exerting its anti-inflammatory effects in a mouse model of TPA-induced ear edema [3].
1-Dodecylimidazole (N-Dodecylimidazole) is a lysosomotropic detergent and a cytotoxic agent. 1-Dodecylimidazole causes cell death by its acid-dependent accumulation in lysosomes, disruption of the lysosomal membrane, and releaseof cysteine proteases into the cytoplasm. 1-Dodecylimidazole has hypocholesterolaemic activity and broad-spectrum antifungal activity[1][2][3].
Chlorobutanol is a pharmaceutical preservative with sedative-hypnotic actions. Chlorobutanol is active against a wide variety of Gram-positive and Gram-negative bacteria, and several mold spores and fungi[1][2].
Isavuconazole is a moderate inhibitor of CYP3A4 and a water-soluble triazole with broad-spectrum antifungal activity.
Oxychloroaphine could be isolated from the bacterium Pantoea agglomerans naturally present in soil. Oxychloroaphine has broad-spectrum antifungal activity. Oxychloroaphine has cytotoxicity in a dose-dependent manner and induces apoptosis. Oxychloroaphine can be used in research of cancer[1][2].
Tofacitinib-d3 (citrate) is deuterium labeled Tofacitinib (citrate). Tofacitinib citrate is an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.
L-Diguluronic acid disodium is a linear polysaccharide copolymer composed of two L-guluronic acid. L-Diguluronic acid disodium can be used to form Alginate. L-Diguluronic acid disodium is a generic name of unbranched polyanionic polysaccharides and it can be used for the research of antifungal agents delivery carries[1].
Cyprodinil-13C6 is the 13C6 labeled Cyprodinil. Cyprodinil is an anilinopyrimidine broad-spectrum fungicide that inhibits the biosynthesis of methionine in phytopathogenic fungi. Cyprodinil inhibits mycelial cell growth of B. cinerea, P. herpotrichoides, and H. oryzae on amino acid-free media (IC50s=0.44, 4.8, and 0.03 µM, respectively). Cyprodinil acts as an androgen receptor (AR) agonist (EC50=1.91 µM) in the absence of the AR agonist DHT and inhibits the androgenic effect of DHT (IC50=15.1 µM).
Ulopterol is a coumarin isolated from the leaves of Toddalia asiatica (L.) Lam with potent antibacterial and antifungal activities[1].
Miconazole Nitrate is an imidazole antifungal agent.Target: AntifungalMiconazole is an imidazole antifungal agent, developed by Janssen Pharmaceutica, commonly applied topically to the skin or to mucous membranes to cure fungal infections. It works by inhibiting the synthesis of ergosterol, a critical component of fungal cell membranes. It can also be used against certain species of Leishmania protozoa which are a type of unicellular parasite that also contain ergosterol in their cell membranes. In addition to its antifungal and antiparasitic actions, it also has some antibacterial properties. Miconazole is also used in Ektachrome film developing in the final rinse of the Kodak E-6 process and similar Fuji CR-56 process, replacing formaldehyde. Fuji Hunt also includes miconazole as a final rinse additive in their formulation of the C-41RA rapid access color negative developing process. From Wikipedia.
Itraconazole-d5 (R51211-d5) is the deuterium labeled Itraconazole. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects[1][2][3].
Luotonin A is an antiviral and antiphytopathogenic fungus agent. Luotonin A has good antiviral activity against tobacco mosaic virus (TMV). Luotonin A also has certain inhibitory activity on topoisomerase I and topoisomerase II. Luotonin A shows antitumor activity[1][2].
Fosetyl-aluminum (Fosetyl-Al) is an active ingredient in many fungicides against downy mildew. Fosetyl-aluminum is used to control many diseases caused by Phytophthora spp. on agricultural and horticultural crops[1][2].
EP3 is an antimicrobial peptide. EP3 has antibacterial and antifungal activities. EP3 inhibits E. gallinarum, P. pyocyanea, A. baumanii, K. terrigena with a MIC value of 12.85 μg/mL. EP3 also shows antitumor activity against cancer cells, and induces cell apoptosis[1].
Prothioconazole is a triazolinthione fungicide. Prothioconazole is a CYP51 inhibitor[1].
4',6,7-Trimethoxyisoflavone is an isoflavone with antimicrobial activities against a wide range of bacteria and fungi. 4',6,7-Trimethoxyisoflavone also has antioxidant effects[1].
Terbinafine hydrochloride (TDT 067 hydrochloride) is an antifungal medication used to treat fungal infections. It is a potent non-competitive inhibitor of squalene epoxidase from Candida with a Ki of 30 nM.