Microbiology/Virology

<p>NNRT-IN-5 (compound 10d) is an orally available non-nucleoside reverse transcriptase (Reverse Transcriptase) inhibitor.</p>

<p>ZIKV-IN-5 is an acid-stable, low cytotoxic anti-ZIKV agent with an EC50 value of 0.71 μM. ZIKV-IN-5 showed effective inhibition of ZIKV NS5 MTase activity.</p>

<p>Urease-IN-2 is a non-competitive inhibitor of urease (IC50: 0.94 μM, Ki: 1.6 μM) that non-competitively inhibits Jack bean urease (JBU).</p>

<p>Anti-Trypanosoma cruzi agent-1 (Compd E5) has a potent anti-Toxoplasma effect.</p>

<p>YKL-04-085 inhibits viral translation effectively, with strong antiviral action at much lower doses than those affecting host-cell growth.</p>

<p>MIV-150 is a nonnucleoside inhibitor of reverse transcriptase (NNRT). MIV-150 also blocking HIV-1 and HIV-2 infections (EC50&lt;1 nM against HIV-1/HIV-2MN).</p>

<p>LpxH-IN-2 (compound 014), a potent inhibitor of LpxH, exhibits antibacterial activity against E. coli.</p>

<p>Adafosbuvir has antiviral activity.</p>

<p>NBTIs-IN-4, a broad-spectrum Gram-positive antibacterial, inhibits DNA rotamases/topoisomerase IV, with low resistance.</p>

<p>NRTT-IN-1 (Compound 1) is an inhibitor of the nucleoside reverse transcriptase translocation (NRTT), effectively blocking HIV DNA synthesis and viral replication.</p>

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

<p>Xeruborbactam isoboxil is a β-lactamase (beta-lactamase) inhibitor.</p>

<p>Gln-AMS (TFA) is a type Ia amido-tRNA synthetase (AARS) inhibitor with a Ki value of 1.32 μM for glutaminyl-tRNA synthetase.</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>Aztreonam-siderophore conjugate 63 is an antibacterial agent that exhibits efficacy against Gram-negative bacteria through the linkage of aztreonam to a</p>

<p>Neocryptolepine-Cl (compound Z24) is an inhibitor of Bcthi4, demonstrating excellent antifungal activity against B. cinerea, with an EC50 value of 0.56 μg/mL.</p>

<p>Jun13296 is an orally active quinoline SARS-CoV-2 papain-like protease inhibitor (IC50 = 0.13 µM, Ki = 8.8 nM). It demonstrates potent inhibitory effects against SARS-CoV-2 variants and Nirmatrelvir-resistant mutants. Jun13296 reduces lung viral titers and prevents lung tissue damage in SARS-CoV-2 infection models.</p>

<p>KKL-40 is a small-molecule inhibitor that targets the trans-translation process, effectively suppressing methicillin-sensitive and resistant Staphylococcus aureus (S. aureus) and other Gram-positive pathogens, including vancomycin-resistant Enterococcus faecium, Bacillus subtilis, and Streptococcus pyogenes. It works in synergy with the human antimicrobial peptide LL-37 to inhibit S. aureus, but does not show synergistic effects with other antibiotics such as daptomycin, kanamycin, or erythromycin. KKL-40 inhibits trans-translation, an extreme form of recoding, while being non-toxic to HeLa cells.</p>

<p>VPC-80051 is an hnRNP A1 splicing activity inhibitor that directly interacts with the hnRNP A1 RBD and reduces AR-V7 messenger levels in the 22Rv1 CRPC cell line. VPC-80051 is applicable in prostate cancer research.</p>

<p>Atramycin A is an anthraquinone antibiotic with antitumor properties.</p>

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

<p>MED6-189, an analog of kalihinol, disrupts the apicoplast functions and vesicular transport in the malignant malaria parasite (P. falciparum, IC50 &lt; 50 nM). The compound specifically targets the apicoplast, which is a non-photosynthetic plastid essential for isoprenoid synthesis, found in most apicomplexan parasites.</p>

<p>Antifungal agent 39 (Compound 9h) is a broad-spectrum antifungal agent.</p>

<p>NSC 641396 is a ribonucleotide reductase (RNR) inhibitor with an IC50 value of 1.2 μM. Additionally, it acts as an inhibitor of protein arginine N-methyltransferase 9 (PRMT9) and exhibits antitumor properties.</p>

<p>Compound 5q is a potent antitubercular with low MIC90 values (0.40-23.51 μg/mL) against M. tuberculosis strains, showing minimal cytotoxicity.</p>

<p>LpxC-IN-10 is a selective LpxC inhibitor with an MIC of 0.5 μg/mL against E. coli and K. pneumoniae and is capable of being used to study bacterial infections.</p>

<p>GHP-88309 is an orally active, broad-spectrum anti-paramyxovirus agent that targets viral polymerase, interrupting viral RNA synthesis. It effectively inhibits respiratory syncytial virus (RSV), measles virus (MeV), and canine distemper virus (CDV) with an EC50 of 0.06-1.2 μM. In mouse models, GHP-88309 demonstrates significant anti-infective activity.</p>

<p>Zorubicin, a Daunorubicin derivative, targets topoisomerase II, inhibits DNA polymerase, and researches acute leukemia, sarcomas.</p>

<p>Antibacterial agent 118, potent against various mycobacteria, has MIC values ranging from 10.2 to 163.0 μM. Useful in TB research.</p>

<p>Antifungal agent 13 demonstrates significant antifungal activity against Sclerotinia sclerotiorum, achieving an EC50 of 1.25 mg/L.</p>

<p>Pneumolysin-IN-1 (compound PB-3), characterized as a targeted small molecule inhibitor of Pneumolysin (PLY) with an IC50 value of 3.1 µM, acts as a pore-blocking agent and an anti-virulence factor. This compound is useful for researching infections caused by Streptococcus pneumoniae [1].</p>

<p>Metallo-β-lactamase-IN-16 (compound 18), a sulfone-containing metallo-β-lactamase inhibitor, exhibits antimicrobial activity. It effectively inhibits various metallo-β-lactamases, including NDM-1 (New Delhi metallo-β-lactamase-1), IMP-1 (imipenemase-1), VIM-1 (Verona Integron-encoded Metallo-β-lactamase), and VIM-2. The IC50 values for these enzymes are 0.16 nM, 0.23 nM, 0.31 nM, and 1.0 nM respectively.</p>

<p>Antifungal agent 17 showed good antifungal activity against B. cinerea (EC50: 2.86 μg/mL).</p>

<p>Anti-MRSA agent 23 (compound 11) is a potent agent against methicillin-resistant Staphylococcus aureus. This compound exhibits both antibacterial and antibiofilm properties. It facilitates the healing and reconstruction of MRSA-infected skin wounds by reducing bacterial load, alleviating inflammation, and promoting angiogenesis.</p>

<p>GSK_WRN4 is a WRN helicase inhibitor with anti-cancer activity, inhibiting MSI tumor cell growth by inducing DNA double-strand breaks, useful in cancer research</p>

<p>ACSS2-IN-1, a potent ACSS2 inhibitor, has IC50 0.01-&lt;1 nM; useful in cancer research.</p>

<p>Aurantiogliocladin is a mild antibiotic effective against Staphylococcus epidermidis, but it shows no efficacy against Staphylococcus aureus. It is also capable of inhibiting biofilm formation.</p>

<p>MRL-494, a small-molecule BamA inhibitor, resists efflux and outer membrane permeability, with antibacterial properties.</p>

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

<p>MsbA-IN-1: Potent MsbA inhibitor (IC50: 4 nM), anti-E. coli (MIC: 79 μM), penetrates Gram-negative bacteria.</p>

<p>BMIM-TFSI (compound8) is an HIV-1 integrase inhibitor that effectively suppresses both the 3'-processing (3'-P) and strand transfer (ST) steps of the integration process. It is applicable in HIV-1 research.</p>

<p>ddCTP trisodium, an HIV reverse transcriptase target, aids AIDS research and DNA sequencing as a ddNTP.</p>

<p>Potent, selective CHS inhibitor with 0.12 mM IC50; effective against drug-resistant fungi.</p>

<p>ALG-000184, a prodrug of the potent HBV capsid assembly modulator ALG-001075, shows potential for use in HBV infection research.</p>

<p>MsbA-IN-4 (Compound 32) is a highly selective and potent inhibitor of MsbA (IC50: 3 nM).MsbA-IN-4 inhibits Escherichia coli (MIC: 12 μM).</p>

<p>PKZ18 is an antibiotic that inhibits bacterial growth with a MIC value of 32-64 μg/mL against most Gram-positive bacteria. It suppresses the in vivo transcription and translation of glycyl-tRNA synthetase mRNA. PKZ18 selectively targets stem I specifier loops in Gram-positive bacteria, directly reducing T-box transcription readthrough of associated genes. It prevents codon-anticodon pairing necessary for tRNA binding and is less likely to induce resistance.</p>

<p>Diploicin is a dibenzofuran lactone compound with activity against Gram-positive bacteria, found in lichens (lichens).</p>

<p>Potent CHS inhibitor with an IC50 of 0.10 mM; exhibits broad-spectrum antifungal properties.</p>

<p>Antibacterial agent 81 blocks DNA transcription, targets S. aureus (MIC 12.5μM) &amp; M. smegmatis (MIC 7.8μM). Used in infection research.</p>

<p>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.</p>