Microbiologie/Virologie

Antitubercular agent-15 (5n): low toxicity, fights M. tuberculosis strains; MIC90 values range 0.73-18.8 μg/mL.

MBX-1162, a bis-indole compound, has demonstrated unique substrate specificity related to MepA and MepR in studies investigating its resistance mechanisms in Staphylococcus aureus. It has not shown cross-resistance with related compounds.

OPC-167832: oral dprE1 inhibitor, IC50 0.258 μM, anti-tuberculosis, for Mycobacterium tuberculosis research.

Antiviralagent 67 (compound PC6) is an inhibitor of DENVNS5 (RNA-dependent RNA polymerase) with a Ki value of 1.12 nM.

Artefenomel (OZ439) is an orally active anti-malarial ozone analog with antiviral activity for the study of SARS-CoV-2 infections and malaria infections.

(-)-15-Deoxyspergualin is a potent antitumor agent that demonstrates significant inhibition against mouse leukemia L-1210.

N'-(2-Fluorophenyl)pyrazine-2-carbohydrazide is a Ole1p desaturase inhibitor as well as antifungal agent [1].

HIV-IN-3 (Compound 22a) is a potent inhibitor of HIV (IC50: 1.5 μM). HIV-IN-3 has potential for the study of HIV-related diseases.

PqsR-IN-2, potent PqsR inhibitor, curbs Pseudomonas aeruginosa communication, reduces pyocyanin, with low toxicity.

CYP2C19-IN-1: potent CYP2C19 inhibitor, non-genotoxic, non-hepatotoxic, blocks RdRP (Ki: 6.16 μM), useful for ZIKV research.

Mpro inhibitor blocks MHV-A29, HCoV-229E, FOPV (IC50: 2.7–8.8 μM), and SARS-CoV-2 (IC50: 16.8 μM) in plaque assays.

Apalcillin (PC-904) combined with Ro 48-1220 (a penicillin sulfone β-lactamase inhibitor) exhibits broad-spectrum activity against Gram-negative aerobic and anaerobic bacteria, excluding Klebsiella acid-producing strains. This combination shows strong efficacy against β-lactamase-producing Moraxella catarrhalis, Haemophilus influenzae, and Neisseria gonorrhoeae with an effective MIC of 11 μg/mL. Additionally, it inhibits Pseudomonas aeruginosa, Stenotrophomonas maltophilia, and Acinetobacter at low MICs (0.25 to 4 μg/mL). However, it has limited efficacy against oxacillin-resistant staphylococci and some Gram-positive bacteria. Apalcillin/Ro 48-1220's effectiveness against certain extended-spectrum β-lactamase-producing Escherichia coli is comparable to piperacillin/tazobactam, though it is less effective against SHV-type β-lactamases.

G092 is a potent inhibitor of MsbA. MsbA is an ABC transporter protein. G092 has potential for antibacterial drug research.

MraY-IN-2 (compound 6) is an effective inhibitor of bacterial transposase MraY (IC50=4.5 μ M), and can be used for antibacterial research.

Adafosbuvir has antiviral activity.

Isazofos is a broad-spectrum organophosphate insecticide and nematicide effective in controlling a variety of lawn pests, such as nematodes (Radopholus similis). It also demonstrates efficacy in managing rice gall midge.

Cap-dependent endonuclease-IN-6 (compound 13) is a Cap-dependent endonuclease (CEN) inhibitor that inhibits influenza virus.

MLEB-22043 is a synthetic siderophore-monocyclic β-lactam conjugate which enters bacteria through TonB-dependent transport proteins utilizing its siderophore component, subsequently exerting antibacterial activity via its β-lactam portion. This compound acts as a broad-spectrum antibiotic, exhibiting significant inhibitory activity against pathogens such as Klebsiella pneumoniae, Escherichia coli, Acinetobacter baumannii, and Pseudomonas aeruginosa.

SARS-CoV-2-IN-106 (compound 19) is a SARS-CoV-2 papain-like protease inhibitor, displaying IC50 values of 0.44 μM for papain-like proteases and 0.18 μM for viral replication.