antifungal agent 1

Antifungal agent 1 is an effective antifungal agent.

Antifungal agent 100 (compound 3i) demonstrates notable antifungal activity, exhibiting an EC 50 of 0.33 mg/L against S. sclerotiorum. It also possesses an IC 50 value of 0.63 mg/mL targeting the Succinate dehydrogenase (SDH) of the same organism [1].

Antifungalagent 109 (compound F) is a spirorings [thiazolidinone] compound with antifungal properties, exhibiting inhibition zones of 10-17 mm.

Antifungal agent 114 (Compound 19g) serves as an inhibitor of Cytochrome P450 (Cytochrome P450), effectively suppressing CYP2C9, CYP2C19, CYP2D6, and CYP3A4 at 10 μM. It exhibits antifungal activity against Cryptococcus neoformans, Candida, and Aspergillus, with an MIC of less than 0.0625 μg/mL. Additionally, Antifungal agent 114 demonstrates favorable metabolic stability in human liver microsomes with a half-life of 107 minutes.

Antifungalagent 117 is a bipyrrole carboxamide derivative with antifungal activity, exhibiting an EC50 value of 11.58 mg/L against Sclerotinia sclerotiorum. This compound induces cell death by increasing cell membrane permeability, causing an imbalance in osmotic pressure between the interior and exterior of the cell. It also promotes oxidative damage to the cell membrane by inducing the accumulation of reactive oxygen species (ROS), leading to the leakage of cellular contents. RNA sequencing analysis has demonstrated that Antifungalagent 117 disrupts cell membrane structure by downregulating catalase genes and upregulating neutral ceramidase genes, accelerating ceramide metabolism and hastening cell death. The compound holds significant potential for application in plant protection and the control of fungal infections.

Antifungalagent 110 exhibits antifungal activity against Botrytis cinerea and Rhizoctonia solani. It demonstrates significant effectiveness in inhibiting R. solani, with an EC50 value of 0.27 mg/L. Antifungalagent 110 shows promise for use in plant disease research.

Antifungalagent 116 (compound 1a) exhibits broad-spectrum antifungal (fungal) activity.

Antifungalagent 115 (compound 8n) is a non-competitive inhibitor of chitin synthase (CHS), displaying an IC50 of 93 µM. It exhibits both broad-spectrum antifungal activity and significant efficacy against resistant fungi. Antifungalagent 115 is useful for studies on fungal infections.

Antifungalagent 123 (Compound 4b) demonstrates strong affinity for the oxidoreductase of Staphylococcus aureus or membrane proteins of Candida albicans, exhibiting both antibacterial and antifungal properties. Additionally, it is capable of scavenging free radicals, showcasing antioxidant effects. Antifungalagent 123 also inhibits the TLR signaling pathway and possesses anti-inflammatory activity.

Antifungalagent 125 (compound 4H) is a potent succinate dehydrogenase (SDH) inhibitor with an IC50 of 3.59 μg/mL and exhibits fungicidal activity against Alternaria alternata.

Antifungalagent 257 (Compound 7e) is a broad-spectrum antifungal agent with an EC50 value of 4.15 μM against F. graminearum.

Antifungalagent 128 (Compound 3ja) is an antifungal agent that, in combination with Fluconazole, has a MIC range of 0.5-4 μg/mL against C. albicans strains. It is applicable in the study of anti-infective therapies.

Antifungalagent 127 (Compound 6c) is an antifungal agent with potent inhibitory activity against Botrytis cinerea and Rhizoctonia solani.

Antifungalagent 129 (Compound 4g) acts as an inhibitor against Rhizoctonia solani, with an EC50 value of 4.27 mg/L. It shows effective control of rice sheath blight in both in vitro and in vivo studies. Preliminary investigations using scanning electron microscopy, molecular docking, enzyme activity assays, and cytotoxicity tests suggest that Antifungalagent 129 may exert its inhibitory action by affecting the cell structure or physiological processes of Rhizoctonia solani. This compound has potential applications in agricultural research related to plant diseases caused by Rhizoctonia solani, such as rice sheath blight.

Antifungalagent 131 (compound A20) is an antifungal agent with a minimum inhibitory concentration (MIC) of 64 μg/mL. When used in combination with Fluconazole, it demonstrates exceptional antifungal potential.

Antifungalagent 132 (compound 25) is a selective and potent antifungal agent. It inhibits Cryptococcus neoformans May1 with a Ki value of 180 pM.

Antifungalagent 130 (Compound A7) is an orally active antifungal agent exhibiting significant inhibitory activity against Candida glabrata [MIC= 0.12 ng/mL] and Cryptococcus neoformans [MIC= 0.12 ng/mL]. It effectively disrupts fungal cell iron homeostasis and induces oxidative stress, leading to antifungal effects. Additionally, Antifungalagent 130 inhibits the formation of fungal virulence factors, such as biofilms, capsules, urease, and melanin. This compound shows strong antifungal properties, making it suitable for research on drug-resistant fungal infections.

Antifungalagent 103 (compound 7y) is a potent antifungal agent that inhibits R. solani with an EC50 value of 0.47 μg/mL.

Antifungalagent 102 (compound C20) is an agent effective against gray mold with an EC50 value of 1.23 μg/mL.

Antifungalagent 104 (Compound 5e) exhibits antifungal activity against Sclerotinia sclerotiorum, Rhizoctonia solani, and Botrytis cinerea, with EC50 values of 1.52 μg/mL, 0.06 μg/mL, and 15.69 μg/mL, respectively. Additionally, Antifungalagent 104 has low cytotoxicity towards human kidney cells 239A, within the range of 6.28-100 mM.

Antifungalagent 134 (Compound B13) is an antifungal agent effective against Botrytis cinerea, Alternaria solani, Fusarium graminearum, Rhizoctonia solani, Colletotrichum orbiculare, and Alternaria alternata with EC50 values of 3.24, 1.89, 1.70, 0.36, 4.27, and 1.50 μg/mL, respectively. It disrupts the fungal cell membranes and mitochondria, leading to substantial accumulation of reactive oxygen species (ROS). Additionally, Antifungalagent 134 exhibits significant herbicidal activity on field weeds such as Amaranthus retroflexus L and Abutilon theophrasti Medicus, and is applicable in crop disease and field weed research.

Antifungalagent 133 (compound D2) is an orally active antifungal compound with an MIC80 value of 0.13 µg/mL against C. neoformans H99. It is suitable for research on cryptococcal meningitis.

Antifungal agent 18 is a new antifungal compound used for treating fungal infections.

Antifungal agent 15 exhibits remarkable potency, with EC50 values of 0.52 and 0.50 μg/mL against S. sclerotiorum and B. cinerea, respectively.