fungicidal

Taurolidine is a synthetic taurine analog with antimicrobial and anti-neoplastic actions. It displays broad bactericidal and fungicidal activity.

DDAC (Quaternium 12), also known as Didecyldimethylammonium chloride, is a dialkyl-quaternary ammonium compound widely utilized in various products due to its bactericidal, virucidal, and fungicidal characteristics.

Hexetidine (NSC-17764) is a bactericidal and fungicidal antiseptic. It is used as a 0.1% mouthwash for local infections and oral hygiene.

2'-Hydroxychalcone is a drug synthesis intermediate for the synthesis of flavonoids. 2'-Hydroxychalcone loaded in nanoemulsion showed fungicidal activity against Coccidioides parapsilosis in Danio rerio model.2'-Hydroxychalcone induced cytotoxicity through oxidative stress in lipid-loaded Hepg2 cells.2'-Hydroxychalcone inhibited the induction of ICAM-1, VCAM-α, tumor necrosis factor-α, and tumor necrosis factor-alpha as determined by reverse transcription-polymerase chain reaction determined by tumor necrosis factor-alpha induces steady-state transcript levels of ICAM-1, VCAM-1, and E-selectin, and therefore may interfere with the transcription of their genes.

Benanomicin A is a microbial metabolite that has been found inActinomycetesand has antifungal, fungicidal, and antiviral activities.1,2It is active against a variety of mammalian and plant pathogenic fungi, includingC. albicans,T. mentagrophytes,C. neoformans,P. oryzae, andA. niger(MICs = 3.13-50 μg/ml).1Benanomicin A inhibits HIV-1 viral infection in MT-4 cells in a concentration-dependent manner.2 1.Takeuchi, T., Hara, T., Naganawa, H., et al.New antifungal antibiotics, benanomicins A and B from an actinomyceteJ. Antibiot. (Tokyo)41(6)807-811(1987) 2.Kondo, S., Gomi, S., Ikeda, D., et al.Antifungal and antiviral activities of benanomicins and their analoguesJ. Antibiot. (Tokyo)44(11)1228-1236(1990)

Sulbentine (Dibenzthione) is an antifungal agent.

Compound 3a (Antifungal agent 62) exhibits potent fungicidal properties, particularly against Fusarium oxysporum f.sp. cucumerinum, and is utilized in antiviral and fungicidal research [1].

5-epi-Jinkoheremol exhibits more potent fungicidal activity than validamycin.

Sphinganine is a synthetic bioactive sphingolipid that inhibits the growth of C. glabrata and C. albicans with a minimum fungicidal concentration (MFC) value of 0.5 μg/ml for both. More commonly, sphinganine is used as an internal standard in the analysis of sphingoid compounds by chromatographic or spectrometric methods.

Compound 3i (Antifungal agent 63) is a fungicidal agent displaying potent activity against Fusarium oxysporum f.sp. cucumerinum and has applications in antiviral and fungicidal research [1].

Coronarin D shows promising antifungal activity against C. albicans in vitro, the minimum inhibitory concentration (MIC) and the minimum fungicidal concentration (MFC) were 2 and 4 mg/mL, respectively; it is active against tested Gram-positive bacteria, i

Histatin 5 inhibits the activity of the host matrix metalloproteinases MMP-2 and MMP-9 with IC50s of 0.57 and 0.25 μM, respectively. Histatin 5 is a human basic salivary peptide with strong fungicidal properties in vitro.

Pecilocin is a fungicidal antibiotic generated by Paecilomyces varioti Bainier var. antibioticus.

Aspyrone is a polyketide fungal metabolite that has been found inAspergillusand has diverse biological activities.1,2It is active against a panel of 13 fungi when used at a concentration of 20 μg/ml and a panel of 21 bacteria in a disc assay when used at a concentration of 100 μg per disc.1Aspyrone (10-1,000 mg/L) is nematocidal againstP. penetrans.2 1.Torres, M., Balcells, M., Sala, N., et al.Bactericidal and fungicidal activity of Aspergillus ochraceus metabolites and some derivativesPestic. Sci.53(1)9-14(1999) 2.Kimura, Y., Nakahara, S., and Fujioka, S.Aspyrone, a nematicidal compound isolated from the fungus, Aspergillus melleusBiosci. Biotech. Biochem.60(8)1375-1376(1996)

Cymoxanil is a fungicidal against plant diseases caused by fungi belonging to the Perenosporales[1]. [1]. Frederique Tellier , et al. Characterization of Metabolites of Fungicidal Cymoxanil in a Sensitive Strain of Botrytis Cinerea. J Agric Food Chem. 2008 Sep 10;56(17):8050-7.

β-Defensin-4 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts. It induces migration of monocytes in vitro when used at a concentration of 10 nM but does not affect migration of neutrophils and eosinophils. β-Defensin-4 (30 μg/ml) stimulates gene expression and production of IL-6, IL-10, CXCL10, CCL2, MIP-3α, and RANTES by keratinocytes. It also stimulates calcium mobilization, migration, and proliferation of keratinocytes when used at concentrations of 30, 10, and 40 μg/ml, respectively. β-Defensin-4 induces IL-31 production by human peripheral blood-derived mast cells in vitro when used at a concentration of 10 μg/ml and by rat mast cells in vivo following a 500 ng intradermal dose. It also inhibits growth of E. coli, P. aeruginosa, and S. aureus with lethal concentration (LC) values of 5, 12, and 15 μM, respectively, of S. carnosus (MIC = 4.5 μg/ml), and of C. albicans with a minimum fungicidal concentration (MFC) value of 7.5 μM.

Xanthoxyletin shows potent antibacterial, fungicidal, and algicidal properties, it also has anticancer, and anti-inflammatory activities. It shows an inhibitory effect on iNOS protein expression at 10 microM, it also can inhibit the synthesis of nitric oxide and the protein expression of tumor necrosis factor-alpha and cyclooxygenase-2. Xanthoxyletin induces S phase arrest and apoptosis in human gastric adenocarcinoma SGC-7901 cells, the effects are associated with the DNA damage, apoptosis through mitochondrial dysfunction, and cell cycle arrest at S phase in a dose-dependent manner, it also can increase the production of reactive oxygen species.

Naftifine Hydrochloride is the hydrochloride salt form of naftifine, an allylamine derivate with synthetic broad-spectrum antifungal activity. Although the exact mechanism through which naftifine hydrochloride exerts its effect is unknown, it appears to selectively inhibit the enzyme squalene 2, 3-epoxidase, thereby inhibiting the biosynthesis of sterol. This results in a decreased amount of sterols, especially ergosterol which is the primary fungal membrane sterol, and a corresponding accumulation of squalene in fungal cells. Naftifine hydrochloride (Naftifine HCl) can be fungicidal as well as fungistatic to yeasts depending on the concentration and the organisms involved.

Phenothiazine (ENT 38) is a class of agents exhibiting antiemetic, antipsychotic, antihistaminic, and anticholinergic activities. Phenothiazines antagonize the dopamine D2-receptor in the chemoreceptor trigger zone (CTZ) of the brain, potentially preventing chemotherapy-induced emesis.

Omiganan-FITC TFA, a compound integrating the bactericidal and fungicidal cationic peptide Omiganan with a fluorescein isothiocyanate (FITC), is under development as a topical gel aimed at preventing catheter-associated infections [1].

Benanomicin B is a microbial metabolite that has been found inActinomycetesand has antifungal, fungicidal, and antiviral activities.1,2It is active against a variety of mammalian and plant pathogenic fungi, includingC. albicans,T. mentagrophytes,C. neoformans, andP. oryzae(MICs = 1.56-50 μg/ml).1Benanomicin B inhibits HIV-1 viral infection in MT-4 cells in a concentration-dependent manner.2 1.Takeuchi, T., Hara, T., Naganawa, H., et al.New antifungal antibiotics, benanomicins A and B from an actinomyceteJ. Antibiot. (Tokyo)41(6)807-811(1987) 2.Kondo, S., Gomi, S., Ikeda, D., et al.Antifungal and antiviral activities of benanomicins and their analoguesJ. Antibiot. (Tokyo)44(11)1228-1236(1990)

Fenamidone is a foliar fungicide used on grapes, ornamentals, potatoes, tobacco, and vegetables. It exerts its fungicidal effects by acting as a Qo inhibitor.

Ibrexafungerp citrate is a triterpenoid antifungal. Similarly to echinocandins, it inhibits the synthesis of 1,3-β-d-glucan. However, it binds to a different site on the enzyme than echinocandins, resulting in limited cross-resistance. Ibrexafungerp exerts concentration-dependent fungicidal activity against Candida species and retains in vitro activity against most fluconazole-resistant strains.

Pinoresinol ((+)-Pinoresinol) has antiinflammatory, hepatoprotective, and fungicidal activities, it can protect pial microcirculation from I-reperfusion injury, to increase nitric oxide release and to reduce oxidative stress preserving pial blood flow distribution; it may exert pharmacologically interesting effects via modulation of the insulin-like signalling pathway in C.elegans. Pinoresinol causes an upregulation of the CDK inhibitor p21(WAF1/Cip1) both at mRNA and protein levels, inhibits NF-kappaB and activating protein 1 (AP-1).

Compound B12 (Antibacterial agent 157) is a fungicidal agent that can impact protein synthesis in Botrytis cinerea. It is utilized in research for controlling gray mold resistance [1].

Antifungal agent 47 (compound 3b) exhibits the most potent and broad-spectrum fungicidal properties, including significant inhibition of respiration and adenosine 5′-triphosphate synthesis, showcasing its potential as an effective fungicide [1].

Compd 3j (Antibacterial agent 149) is a laccase inhibitor that exhibits potent fungicidal activity, particularly useful in researching rice sheath blight [1].

SDH-IN-9 (compound Ip) serves as a potent Succinate Dehydrogenase inhibitor and exhibits fungicidal properties, effectively targeting Fusarium graminearum Schw at an EC50 value of 0.93 μg/mL [1].

Debneyol exhibits more potent fungicidal activity than validamycin.

Gliovirin is a fungal metabolite that has been found inT. harzianumand has fungicidal, antimicrobial and anti-inflammatory activities.1It is active against the plant pathogenic fungusP. ultimum(MIC = 60 ng/ml) and the parasiteT. brucei brucei(IC50= 90 ng/ml), but has no effect on the plant pathogenic fungiR. solani,P. omnivorum,T. basicola,R. arrhizus, andV. dahliaeor the bacteriaB. thuringiensis,P. fluorescens, andX. malvacearumwhen used at concentrations up to 1,000 ng/ml.2,3Gliovirin decreases phorbol 12-myristate 13-acetate (TPA)- and ionomycin-induced increased expression of COX-2 (IC50= 1 μM) and protein levels of IL-2 in Jurkat cells (IC50= 5.2 μM).1 1.Rether, J., Serwe, A., Anke, T., et al.Inhibition of inducible tumor necrosis factor-α expression by the fungal epipolythiodiketopiperazine gliovirinBiol. Chem.388(6)627-637(2007) 2.Howell, C.R., and Stipanovic, R.D.Gliovirin, a new antibiotic from Gliocladium virens, and its role in the biological control of Pythium ultimumCan. J. Microbiol.29(3)321-324(1983) 3.Iwatsuki, M., Otoguro, K., Ishiyama, A., et al.In vitro antitrypanosomal activity of 12 low-molecular-weight antibiotics and observations of structure/activity relationshipsJ. Antibiot. (Tokyo)63(10)619-622(2010)

Y12196, a newly developed succinate dehydrogenase inhibitor (SDHI), demonstrates potent fungicidal effects specifically targeting F. graminearum.

HSP90-IN-9 is a selective and potent HSP90 inhibitor.HSP90-IN-9 exhibits a dose-dependent fungicidal effect.HSP90-IN-9 in combination with FLC inhibits fungal biofilm formation and fungal morphological changes.HSP90-IN-9 downregulates ERG11, CDR1 and CDR2 gene expression and restores resistance to FLC. HSP90-IN-9 downregulates ERG11, CDR1 and CDR2 gene expression and restores FLC resistance.

Carabrone, a botanical bicyclic sesquiterpenic lactone, is a promising fungicidal agent that can effectively control G. tritici.

Lariciresinol is an enterolignan precursor, it possesses fungicidal activities by disrupting the fungal plasma membrane and therapeutic potential as a novel antifungal agent for the treatment of fungal infectious diseases in humans. Dietary lariciresinol

SDH-IN-7 (compound G28) is a potent inhibitor of succinate dehydrogenase (SDH), exhibiting an IC50 value of 26 nM against porcine SDH and possesses fungicidal properties [1].

TMV-IN-6 (Compound 4g) serves as a novel antiviral and fungicidal agent that impedes tobacco mosaic virus (TMV) assembly, functioning by attachment to TMV coat protein (CP) and disrupting the assembly interaction between TMV CP and RNA [1].

Compound 5d (Antifungal Agent 65) exhibits potent fungicidal activity against Fusarium oxysporum f.sp. cucumerinum and is utilized in antiviral and fungicidal research [1].

Antifungal agent 74 (compound 3c), is a potent substance that exhibits excellent fungicidal activity against C. arachidicola and R. solani, functioning by disrupting steroid biosynthesis and ribosome biogenesis in eukaryotes [1].

Compound 5c (Antifungal agent 64) exhibits potent fungicidal activity against Fusarium oxysporum f.sp. cucumerinum and is applicable for research in antiviral and fungicidal domains [1].

FTR1335 is a CaNMT inhibitor (IC50 = 0.49 nM) with good fungal selectivity. CaNMT inhibitors are fungicidal and show antifungal activity against Candida (especially fluconazole-resistant strains). They function by inhibiting N-myristoyltransferase (NMT), which catalyzes the transfer of a C14 fatty acif from myristoyl-CoA to the N-terminal of glycine in many fungal proteins. Without this process, fungi can die. This process also occurs in humans, and as such selectivity is an important characteristic of these drugs.

O-11 is an analog of the fully saturated, 14-carbon fatty acid myristic acid, in which the methylene group at position 11 is replaced with oxygen. It is highly effective and selective at killingTrypanosoma brucei, the protozoan parasite responsible for African sleeping sickness, exhibiting an LD50of less than 1 μM in a cell culture assay.1,2The toxic effects of O-11 appear to be caused by its ability to inhibit the incorporation of a single myristate into the GPI anchor of the variant surface glycoprotein (VSG), a protein critical for evading the host immune response.1O-11 exhibits essentially no anti-fungal activity when assayed usingC. neoformans, but does have a minor inhibitory effect on HIV-1 replication in T-lymphocytes.3 1.Doering, T.L., Raper, J., Buxbaum, L.U., et al.An analog of myristic acid with selective toxicity for African trypanosomesScience2521851-1854(1991) 2.Doering, T.L., Lu, T., Werbovetz, K.A., et al.Toxicity of myristic acid analogs toward African trypanosomesProceedings of the National Academy of Sciences of the United States of America919735-9739(1994) 3.Langner, C.A., Lodge, J.K., Travis, S.J., et al.4-Oxatetradecanoic acid is fungicidal for Cryptococcus neoformans and inhibits replication of human immunodeficiency virus IThe Journal of Biological Chemisty267(24)17159-17169(1992)

Justicidin B, a potent lignan, exhibits anticancer and proapoptotic properties, additionally serving as a bone resorption inhibitor. This compound demonstrates robust antiviral, fungicidal, and antiprotozoal effects, along with a significant inhibition of platelet aggregation.

SDH-IN-8 (compound G40) is a potent inhibitor of succinate dehydrogenase (SDH), demonstrating an IC50 value of 27 nM against porcine SDH and exhibits fungicidal properties [1].

Compound E8 (Antimicrobial agent-24) is a hydrazide with broad-spectrum fungicidal properties, disrupting the plasma membrane's functionality and inducing morphological and subcellular structural changes in mycelia [1].

Omiganan-FITC is a complex of the cationic peptide Omiganan, which possesses bactericidal and fungicidal properties and is under development as a topical gel for preventing catheter-associated infections, and Fluorescein Isothiocyanate (FITC), a fluorescein derivative used for amine labeling [1].