AI Article Synopsis
- Fungal infections are increasingly threatening the healthcare system due to rising resistance to existing antifungal medications, particularly azoles, which are currently the most commonly prescribed but have notable side effects.
- There's a pressing need for new and effective antifungal agents, especially those targeting lanosterol 14α-demethylase (CYP51), a key enzyme in fungal ergosterol biosynthesis and essential for the fungal life cycle.
- The review explores various derivatives, both azole and non-azole based, as potential antifungal agents, focusing on their structure-activity relationships and molecular interactions with CYP51, providing insights for medicinal chemists in developing safer and more effective antifungal treatments.
Article Abstract
Fungal infections are posing serious threat to healthcare system due to emerging resistance among available antifungal agents. Among available antifungal agents in clinical practice, azoles (diazole, 1,2,4-triazole and tetrazole) remained most effective and widely prescribed antifungal agents. Now their associated side effects and emerging resistance pattern raised a need of new and potent antifungal agents. Lanosterol 14α-demethylase (CYP51) is responsible for the oxidative removal of 14α-methyl group of sterol precursors lanosterol and 24(28)-methylene-24,25-dihydrolanosterol in ergosterol biosynthesis hence an essential component of fungal life cycle and prominent target for antifungal drug development. This review will shed light on various azole- as well as non-azoles-based derivatives as potential antifungal agents that target fungal CYP51. Review will provide deep insight about structure activity relationship, pharmacological outcomes, and interactions of derivatives with CYP51 at molecular level. It will help medicinal chemists working on antifungal development in designing more rational, potent, and safer antifungal agents by targeting fungal CYP51 for tackling emerging antifungal drug resistance.
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| http://dx.doi.org/10.1111/cbdd.14266 | DOI Listing |
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