Novel Anti-Fungal Agents

Ref: 10460
Two novel classes of anti-fungal agents that have demonstrated broad spectrum of activity against fungal species with significantly improved properties over existing antifungal compounds

Key advantages
  • Broad spectrum of activity against fungal species
  • High selectivity for fungal PLB
  • Low levels of haemolytic activity and cytotoxicity
  • Broad spectrum of applications
  • Animal trials are ongoing

Background

Invasive fungal infections (mycoses) are associated with high morbidity, mortality and an economic burden, especially in immunocompromised patients.

Despite recent additions of new classes of antifungal agents, the number of currently available drugs for the treatment of fungal infections is limited.

The invention

Top: Bis-Cationic compounds (where X-is a suitable counter-ion) Bottom: Bis-Pyridium compounds.

The core technology is focused on the two newly synthesised classes of compounds identified as bis-cationic compounds and bis-pyridinium compounds.

These compounds have demonstrated broad spectrum antimicrobial activity in a series of established in vitro assays against fungal (Crytococcus, Candida and Aspergillus) and bacterial species (methicillan-resistant S.aureus, vancomycin-resistant Enterococcus and Psuedomonas) including clinically relevant yeasts, moulds and dermatopthytes.

These compounds are importantly active at therapeutically acceptable concentrations and demonstrate high selectivity for fungal PLB, with very low levels of haemolytic activity and cytotoxicity at concentrations many times higher than those required for antimicrobial activity.

The compounds do not merely slow the growth of the fungi and bacterial but kill them outright.

Applications

The compounds are suitable for antifungal therapy and could also be used in consumer products such as disinfectants, medical soaps and shampoos.

Additionally, they have potential as agrochemical fungicides and in the “technical chemistry” sector, i.e. as anti-mould agents added to paints, glues, oils, photographic films, timber treatment and animal feed.

Principal inventors

  • Dr. Fred Widmer
  • Dr. Kate Jolliffe
  • Professor Tania Sorrell

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