Microbiologie/Virologie

<p>Saussureamine C is an inhibitor of H274Y and N294S mutants.</p>

<p>HIV-1 inhibitor-13: oral NNRTI, IC50=0.14μM for HIV-1 RT, effective on resistant strains (EC50=2.85-18nM).</p>

<p>BRL-42715 is an effective inhibitor of bacterial beta-lactamases.</p>

<p>ZIKV-IN-4 is a low cytotoxic, acid-stable anti-ZIKV agent with an EC50 value of 3.49 μM. ZIKV-IN-4 exhibited potent inhibition of ZIKV NS5 MTase.</p>

<p>DHX9-IN-19 (compound 3) is an orally active inhibitor of DHX9, playing a significant role in cancer research.</p>

<p>MAY0132 is a potent and selective EPAC2 inhibitor with an IC50 of 0.4 μM. It significantly inhibits the replication of HMPV, AdV, and RSV, reduces cytokine/chemokine production induced by viral infections, and suppresses NF-κB activation. MAY0132 exhibits antiviral activity and can be used in respiratory virus infection research.</p>

<p>Compound 25b inhibits DENV2/ZIKV NS2B/NS3 proteases; IC50: ZIKV 0.67μM, DENV2 4.38μM.</p>

<p>MsbA-IN-2 is a potent inhibitor of the lipopolysaccharide transporter MsbA and is able to act on E. coli MsbA (IC50: 2 nM).</p>

<p>ABT-072 is a nonnucleoside NS5B polymerase inhibitor and a candidate drug evaluated for treatment of hepatitis C virus.</p>

<p>Neuraminidase-IN-4 inhibits neuraminidase (EC50: 1.59 μM) and has strong anti-H5N1 activity.</p>

<p>1,5-Dideoxy-1,5-imino-D-mannitol is an antibiotic with antibacterial properties.</p>

<p>Meclocycline: a tetracycline antibiotic, inhibits LDH, reduces cell toxicity from mutant huntingtin, doesn't change protein levels in PC12 cells.</p>

<p>Tenellin is a fungal metabolite that inhibits Mg2+-, Ca2+-, and Na+/K+-ATPase activities in erythrocytes. Tenellin is cytotoxic to Sf9 and Sf21 insect cells.</p>

<p>Plevitrexed, an oral TS inhibitor (Ki: 0.44 nM), targets α-folate receptor &amp; reduced folate carrier, treats gastric cancer.</p>

<p>Penethamate hydriodide is a diethylaminoethyl ester prodrug of penicillin, utilized via intramuscular injection to treat mastitis in cattle.</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>RAD51-IN-8 inhibits RAD51-BRCA2 interaction and H4A4 with EC50 of 19 μM; a micromolar PPI inhibitor.</p>

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

<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>

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

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

<p>Alphavirus-IN-1 blocks VEEV (EC50: 0.24 μM) &amp; EEEV (EC50: 0.16 μM), non-toxic, stable in mice plasma.</p>

<p>Ro 24-4383 is a carbamate-linked dual-action antibacterial agent.</p>

<p>Antifungal agent 38, a heterocyclic disulfide, shrinks hyphae and damages cell membranes, causing leakage.</p>

<p>LasR-IN-1 (9g) strongly inhibits LasR, potent vs E. coli, with a 28.13 μM MIC against P. aeruginosa.</p>

<p>Bleomycin Free Base, a glycopeptide antibiotic, halts DNA function and treats solid tumors.</p>

<p>Carbodine is an antiviral targeting CTP synthetase, effective against influenza A0/PR-8/34 and A2/Aichi/2/68.</p>

<p>Anti-MRSA agent 3 targets MRSA with 0.098 μg/ml MIC, low toxicity, binds DNA, and disrupts cell walls/membranes.</p>

<p>CM-728 is an oxazanonaphthoquinone that exhibits cytotoxic and antibacterial properties. It acts as a human peroxidase-1 inhibitor and serves as a source of oxidative stress affecting mitochondrial function.</p>

<p>SARS-CoV-2-IN-22 is a SARS-CoV-2 pseudovirus inhibitor (IC50: 16.96 μM).</p>

<p>L-threo-β-Hydroxyaspartic acid is an amino acid antibiotic with activity against Bacillus subtilis, Xanthomonas oryzae, Mycobacterium phlei, and Botrytis cinerea.</p>

<p>QPX7728 is an of ultra-broad-spectrum boronic acid beta-lactamase.</p>

<p>CEN inhibitor IN-17 targets influenza A/H3N2; IC50: 1.29 μM. From patent CN112898346A, DSC701.</p>

<p>Antifungal agent 19 shows the potent antifungal activity ( EC 50 = 0.72 μM).</p>

<p>HCV-IN-7: potent oral HCV NS5A inhibitor, pan-genotypic, IC50s 3-47 pM, good pharmacokinetics, favorable liver uptake.</p>

<p>XR8-69 is a SARS-CoV-2 PLpro inhibitor. XR8-69 has a low micromolar antiviral effect in SARS-CoV-2 infected human cells.</p>

<p>Ladirubicin, as an anthracyclines analog is the leading compound of alkylcyclines.</p>

<p>OUN58101, also MDK-8101/BI-D, is an RSV L-protein inhibitor with no formal name, first reported in patent WO 2005042530.</p>

<p>CDA-IN-4 (compound VS-24) is an inhibitor of chitin deacetylase (CDA). At a concentration of 100 μg/mL, CDA-IN-4 provides a protective effect of 61.2% against rice blast disease.</p>

<p>2'-(2-Nitrobenzyl)-ATP is an analog of rATP. It acts as a transcription terminator by inhibiting the elongation of RNA chains by T7 RNA polymerase.</p>

<p>HSV-TK substrate is a substrate for HSV-TK with antitumor activity. It induces multi-log cytotoxicity in HSV-TK-expressing and bystander cells.</p>

<p>Novel anti-TB agent 62 is a redox compound with bactericidal activity against active and dormant bacteria.</p>

<p>Arterolane is an antimalarial compound. For against P. falciparum Ro73 and W2, the IC50s are both 1.1 nM.</p>

<p>NEU-1017 serves as a broad-spectrum antiparasitic compound, effectively inhibiting T. brucei, L. major, and P. falciparum with EC50 values of 210 nM, 240 nM, and 3 nM, respectively.</p>

<p>SLU-10906 (Compound 63) is an orally active inhibitor of Cryptosporidium. It demonstrates activity against the parasite in cell-based infection models with an EC50 of 0.19 μM and exhibits no cytotoxicity. SLU-10906 is a promising candidate for research in cryptosporidiosis.</p>

<p>KWR095 is an orally active inhibitor of WRN, demonstrating an IC50 of 0.032 μM against WRN ATPase. It disrupts the double-stranded helicase activity of WRN and inhibits tumor cell proliferation, exhibiting antitumor properties.</p>

<p>Neuraminidase-IN-11 (15e) inhibits H1N1 (IC50: 4.7nM), H5N1 (8.46nM), H5N8 viruses (1.5nM) selectively &amp; potently.</p>

<p>NDM-1 inhibitor-7 (Compound A8) is an NDM-1 inhibitor with an IC50 of 10.284 μM. It restores the ability of meropenem (MEM) to penetrate the cell wall of Gram-negative bacteria and effectively reinstates MEM's antibacterial activity against NDM-1 positive Escherichia coli. Moreover, NDM-1 inhibitor-7 demonstrates significant efficacy in both Galleria mellonella and murine peritonitis infection models.</p>

<p>Aurachin C is a quinoline alkaloid belonging to the isoprenoid class, known for its antimalarial, antifungal, and antibacterial properties. It acts as a selective terminal oxidase inhibitor.</p>