Microbiologie/Virologie

MtDTBS-IN-1 is a notably potent binder (K_D = 57 nM) and inhibitor (K_i = 5 μM) of MtDTBS.

3′-Amino-2′,3′-dideoxy-CTP is an analog of nucleoside triphosphates. It selectively inhibits DNA polymerase β.

HIV-1-IN-86 (compound 6m) is an HIV-1 inhibitor with an EC50 of 0.77 μM, exhibiting antiviral activity.

MB076 is an innovative heterocyclic triazole designed with enhanced plasma stability. It effectively inhibits seven distinct Class C Acinetobacter-derived cephalosporinases (ADCs) β-lactamase variants with K i values less than 1 μM. Additionally, MB076 demonstrates a synergistic effect when combined with various cephalosporins to restore pBCSK(−) susceptibility [1].

DXR-IN-3 is an anti-Toxoplasma DXR inhibitor. It exhibits in vitro activity against the TgDXR enzyme, with an IC50 value of 0.62 μM and a Ki value of 0.19 μM. Furthermore, DXR-IN-3 can inhibit the proliferation of Toxoplasma, displaying an IC50 value of 5.46 μM.

Pyriftalid is a novel insecticide known for its potent inhibitory activity against a variety of pests. It is widely utilized in agriculture to effectively manage crop pests, thereby enhancing both the yield and quality of crops. Additionally, research is exploring the use of Pyriftalid in boosting plant resistance to pests and diseases.

Lentiginosine is a selective amyloglucosidase inhibitor.

Benzisothiazolone is an isothiazolinone fungicide that demonstrates growth inhibitory activity against Escherichia coli ATCC 8739 and yeast NCYC 1354. It is utilized in studies investigating growth inhibition models.

CYP51-IN-7 (compound 1g) is an analogue of Fluconazole and serves as an effective antifungal agent. It exhibits inhibitory activity against Microsporum gypseum and Candida albicans, with MIC80 values of 62.5 ng/mL and 250 ng/mL, respectively.

KL-50, a selective toxin, effectively targets tumors deficient in the DNA repair protein O6-methylguanine-DNA-methyltransferase (MGMT), which corrects O6-alkylguanine lesions. This compound induces both DNA damage response pathways and cell cycle arrest in MGMT-deficient cells, regardless of mismatch repair (MMR) status. KL-50 shows promise in the study of brain tumors lacking MGMT.

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.

Laninamivir trifluoroacetate, a long-acting antiviral, treats and prevents Influenza A and B via nasal spray.

And1 degrader 1 (Compound A15) is a degrader of acidic nucleoplasmic DNA-binding protein 1 (And1) that notably induces degradation of And1 in NSCLC cells. When combined with Olaparib (1 μM), And1 degrader 1 at a concentration of 5 μM effectively inhibits proliferation in A549 and H460 cells. This compound is applicable in cancer research studies.

GSK 932121: potent antimalarial, targets P. falciparum by inhibiting cytochrome bc1 in the electron transport chain.

GR 122222X is an inhibitor of topoisomerase II.

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.

Cefempidone (GR 50692) is a third-generation cephalosporin antibiotic. It exhibits antibacterial activity by inhibiting penicillin-binding proteins involved in the synthesis of bacterial cell walls.

GC-78-HCl is an orally active, non-peptidic SARS-CoV-2 Mpro inhibitor with an enzyme IC50 of 0.19 μM. It exhibits strong anti-coronavirus activity and favorable pharmacokinetic properties.

Antibiofilm agent-4 is a LasR inhibitor, demonstrating optimal antibiofilm and anti-QS (quorum sensing) properties.

Nikkomycin Z (Nikkomycin Z from Streptomyces tendae) is a competitive chitin synthase inhibitor.It inhibitor of the growth of filamentous fungi, insects,