Microbiologia/Virologia

<p>Enpatoran hydrochloride (M5049 hydrochloride) is a TLR7/8 inhibitor with antiviral activity that is used in the study of autoimmune diseases.</p>

Ro 24-4383 is a carbamate-linked dual-action antibacterial agent.

<p>FtsZ-IN-4 is an oral FtsZ inhibitor with strong antibacterial effects and good drug traits, low toxicity (CC50 &gt;20μg/mL).</p>

Hyalodendrin ((+)-Hyalodendrin) acts as a fungal growth inhibitor, specifically targeting wood decay fungi. It exhibits low phytotoxicity and possesses an acute toxicity (LD50) level of 75 mg/kg in mice.

Alphavirus-IN-1 blocks VEEV (EC50: 0.24 μM) & EEEV (EC50: 0.16 μM), non-toxic, stable in mice plasma.

Massarilactone H, a polyketide, is a neuraminidase inhibitor, with an IC 50 of 8.18 µM .

<p>Dencatistat is a highly selective and oral cytidine triphosphate synthase 1 CTPS1 inhibitor specific.CTPS1-IN-2 for B-cell, T-cell lymphomas and solid tumors.</p>

<p>Compound 18a: potent vs. T. brucei (IC50: 0.47 μM), &gt;2x efficacy compared to Nifurtimox, good ADME, binds AT-rich DNA.</p>

Fosmanogepix (APX001) is a broad-spectrum oral antifungal that targets Gwt1 enzyme, transforming into active APX001A in the body.

<p>MK-3402 is a metallo-beta-lactamase inhibitor. MK-3402can be used in the research of bacteria .</p>

Compound 3d: antitubercular, MIC 0.007 μg/mL vs MTB H37Rv, 1.851 μg/mL vs MDR-MTB 16833, metabolically unstable.

<p>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].</p>

<p>Antifungal agent 16 has antimicrobial activity comparable to that of ciprofloxacin and has higher antifungal activity than fluconazole.</p>

Succinate dehydrogenase-IN-8 (compound i19) is a potent inhibitor of succinate dehydrogenase (SDH). This indanoyl amino acid derivative demonstrates strong antifungal activity in vitro against Rhizoctonia solani (EC50 = 0.1843 mg/L), Botrytis cinerea (EC50 = 0.4829 mg/L), and Sclerotinia sclerotiorum (EC50 = 0.1349 mg/L).

<p>FNC-TP trisodium, active intracellular FNC form, inhibits NRTI, fights HIV, HBV, and HCV.</p>

Antitubercular agent-23 combats Candida albicans (MIC: 1.1 μg/ml) and M. tuberculosis (MIC: 1 μg/ml).

<p>RAD51-IN-8 inhibits RAD51-BRCA2 interaction and H4A4 with EC50 of 19 μM; a micromolar PPI inhibitor.</p>

<p>TKB272 is an orally active antiviral agent that selectively targets the main protease (Mpro) of SARS-CoV-2, effectively inhibiting the infection and replication of various strains, including Omicron variants (such as XBB.1.5 and EG.5.1). It exhibits an enzyme inhibitory activity with an IC50 of 0.7 µM against SARS-CoV-2WK-521 Mpro and shows potent antiviral activity at the cellular level with an EC50 as low as 2.6 nM in HeLahACE2-TMPRSS2 cells against the BQ.1.1 strain. TKB272 also has a CC50 of 98 µM, indicating low cytotoxicity. Furthermore, it demonstrates a significant suppression of SARS-CoV-2XBB.1.5 replication in the B6.Cg-Tg(K18-hACE2)2-Prlmn/J transgenic mouse model, suggesting potential use in the research of SARS-CoV-2 infections.</p>

<p>Antimicrobial Agent-29 (Compound C35) influences the interaction between human hemoglobin and the Staphylococcus aureus IsdB hemophore. This compound facilitates the identification of IsdB:Hb PPI inhibitors [1].</p>

Antitubercular agent-22 combats Candida albicans (MIC: 2.34 μg/ml) and M. tuberculosis (MIC: 2 μg/ml).