Fungal organisms are widespread in nature and pose significant challenges to both agricultural and human health sectors. Unlike the development of new antibacterial drugs, antifungal drug development is more complex since fungi are eukaryotes, and many potential molecular targets are also present in humans, increasing the risk of host toxicity and harmful side effects. Currently, approved antifungal drugs have critical limitations, in particular the development of resistance and undesirable complications. Thus, it is obvious that there exists an urgent demand for novel antifungal agents.
Life Chemicals has designed a dedicated Antifungal Library of over 4,000 drug-like screening compounds, which are potential antifungal agents.
Please, contact us at orders@lifechemicals.com for any additional information and price quotations.
The compound selection can be customized based on your requirements, cherry picking is available.
Background information
Fungal infections are notoriously challenging to diagnose and treat, making them a leading cause of global mortality and morbidity. They are responsible for at least 1.5 million deaths annually worldwide, particularly affecting immunocompromised individuals undergoing aggressive therapies or suffering from conditions such as HIV/AIDS. Notably, approximately 90 % of these deaths result from fungal species within the Aspergillus, Candida, Cryptococcus, Mucor, Pneumocystis, and Rhizopus genera [1].
The currently available antifungal agents can be broadly categorized into several groups, including inhibitors of ergosterol biosynthesis, disruptors of fungal membranes, inhibitors of fungal cell wall synthesis, inhibitors of sphingolipid biosynthesis, nucleic acid synthesis inhibitors, inhibitors of protein biosynthesis, and inhibitors of microtubule biosynthesis [1]. However, the therapeutic options for treating invasive fungal infections are quite limited, primarily consisting of just three structural classes of antifungal drugs: polyenes, azoles, and echinocandins.
Compound selection
The screening compound set was prepared based on the proprietary HTS Compound Collection. A 2D fingerprint similarity search (Tanimoto 80 % cut-off) was performed against a reference set of 21,450 molecules with reported antifungal activity (activity data threshold < 10 μM, extracted from ChEBI, BindingDB and ChEMBL databases) against different fungi species:
- Agaricus bisporus
- Ajellomyces capsulatus
- Alternaria (A. alternata, A. kikuchiana, A. mali, A. solani, A. tenuis, A. benhamiae)
- Arthroderma (A. cajetani, A. otae)
- Ascochyta
- Aspergillus (A. clavatus, A. flavus, A. fumigatus, A. niger, A. ochraceus, A. oryzae, A. parasiticus)
- Athelia rolfsii
- Bionectria ochroleuca
- Bipolaris oryzae
- Blumeria graminis
- Botryosphaeria dothidea,
- Botryotinia fuckeliana
- Candida (C. albicans, C. dubliniensis, C. glabrata, C. parapsilosis, C. sake, C. tropicalis)
- Ceratobasidium cereale
- Ceratocystis paradoxa
- Cercospora beticola
- Cladosporium (C. cladosporioides, C. sphaerospermum)
- Clavispora lusitaniae
- Cochliobolus heterostrophus,
- Cochliobolus lunatus
- Cochliobolus pallescens
- Colletotrichum (C. capsica, C. coccodes, C. gloeosporioides, C. lindemuthianum, C. truncatum)
- Corticium
- Corynespora cassiicola
- Cryphonectria parasitica
- Cryptococcus (C. gattii, C. neoformans)
- Cyberlindnera jadinii
- Cytospora
- Diaporthe longicolla
- Diplodia seriata
- Emericella nidulans
- Encephalitozoon cuniculi
- Epidermophyton floccosum,
- Fusarium (F. culmorum, F. decemcellulare, F.equiseti, F.graminearum, F.oxysporum, F.solani, F.udum)
- Galactomyces geotrichum
- Gibberella (G. fujikuroi, G. intermedia, G. moniliformis, G. zeae)
- Gloeophyllum trabeum
- Glomerella (G. acutata, G. cingulate, G. tucumanensis)
- Helminthosporium
- Hypocrea (H. koningii, H. lixii, H. rufa)
- Kluyveromyces marxianus
- Laetiporus sulphureus
- Lasiodiplodia theobromae
- Lenzites betulinus
- Leptosphaeria maculans
- Macrophomina phaseolina
- Magnaporthe (M. grisea, M. oryzae)
- Meyerozyma guilliermondii
- Microdochium nivale
- Microsporum gypseum
- Monilinia laxa
- Monographella nivalis var. nivalis
- Mycogone perniciosa
- Mycosphaerella arachidis
- Neofusicoccum (N. luteum, N. ribis)
- Oculimacula (O. acuformis, O. yallundae)
- Penicillium (P. crustosum, P. expansum, P. italicum, P. marneffei)
- Pestalotiopsis microspora
- Phomopsis (P. asparagi, P. obscurans)
- Physalospora pyricola
- Pichia (P. kudriavzevii, P. norvegensis)
- Pleurotus ostreatus
- Pneumocystis (P. carinii, P. jirovecii)
- Podosphaera (P. fuliginea, P. xanthii)
- Puccinia recondita
- Rhizoctonia (R. bataticola, R. solani)
- Rhizomucor
- Rhizopus oryzae
- Saccharomyces cerevisiae
- Sclerotinia sclerotiorum
- Scopulariopsis
- Sporothrix schenckii
- Syncephalastrum racemosum
- Thanatephorus cucumeris
- Thielaviopsis basicola
- Trametes versicolor
- Trichoderma hamatum
- Trichophyton (T. interdigitale, T. mentagrophytes, T. rubrum, T. tonsurans, T. violaceum, T. asahii)
- Valsa mali
- Verticillium (V. albo-atrum, V. dahlia)
- Villosiclava virens
Representative screening compounds from the Antifungal Screening Compound Library
References
S. Campoy and J. L. Adrio, “Antifungals,” Biochem. Pharmacol., vol. 133, pp. 86–96, 2017, doi: 10.1016/j.bcp.2016.11.019.