antifungal agent 20

Antifungal agent 20 demonstrates significant antifungal efficacy against a range of fungal pathogens including Colletotrichum gloeosprioides, Rhizoctonia solani, Phytophthora nicotianae var. nicotianae, Diplodia pinea, Colletotrichum acutatum, and Fusarium oxysporum f. sp. niveum.

CYP51-IN-20 (compound 5b), an antifungal agent, effectively inhibits CYP51 and exhibits significant activity against Candida albicans ATCC 10231. It suppresses the ERG11 (Cyp51) gene expression and markedly curtails the morphological transformation from yeast to hyphae. Furthermore, when combined with Voriconazole, CYP51-IN-20 synergistically occupies the entire CYP51 binding site, enhancing its inhibitory impact in the Glechoma moth model.

SDH-IN-20 (compound A19) is an antifungal agent that exhibits remarkable efficacy against Verticillium dahliae and R. solani, with EC50 values below 3.0 μg mL and 2.87 μg mL, respectively. It functions as a potent succinate dehydrogenase (SDH) inhibitor, with an IC50 value of 29.33 μM, and significantly disrupts the cell membrane integrity and hyphal morphology of R. solani.

Heronamide C, a polyketide macrolactam antifungal agent synthesized by marine Actinomycetes, exhibits selective toxicity by inhibiting growth and promoting abnormal cell wall material accumulation in wild-type fission yeast cells (MIC = 0.13-0.28 μM), without affecting Gram-positive bacteria or human cancer cell lines, HeLa and MDA-MB-231. At 20 μM, it triggers reversible morphological alterations, notably the development of large intracellular structures, in HeLa cells.