Microbiologie/Virologie

<p>SARS-CoV-IN-6 (Compound 17) acts as an inhibitor of SARS-CoV-1 and SARS-CoV-2 RdRp, demonstrating an IC50 value of 7.8 μM against SARS-CoV-2 RdRp. This compound reduces the cytopathic effects of single-round infectious particles (SRIP) infected with SARS-CoV-1 and SARS-CoV-2 replicons and inhibits the expression of SARS-CoVN proteins. The EC50 values for SRIP based on SARS-CoV-1 and SARS-CoV-2 replicons are 0.12 µM and 1.47 µM, respectively.</p>

<p>(E)-Cefodizime ((E)-THR-221) is an antibiotic that selectively binds to penicillin-binding proteins (PBPs), inhibiting bacterial cell wall synthesis, which results in its antibacterial activity. It holds potential for research into various bacterial infections, including the prevention of preoperative infections.</p>

<p>SARS-CoV-2 Mpro-IN-44 (Compound 25) is a broad-spectrum inhibitor of the main protease (Mpro) for coronaviruses. It exhibits inhibitory activity against several high-risk coronaviruses, including SARS-CoV-2 and PEDV, with an IC50 of less than 0.6 μM. The broad inhibition of coronaviruses by SARS-CoV-2 Mpro-IN-44 is achieved through enhanced interaction with conserved sites of Mpro. This compound is a potential candidate for the development of antiviral drugs against coronaviruses.</p>

<p>Omaciclovir (ABT-091) is a herpesvirus herpesvirus replication inhibitor with antiviral activity that is used in the study of herpesvirus infections.</p>

<p>Saroaspidin B is a dimeric form of a biphenyl triphenol, characterized as an antibiotic compound.</p>

<p>APE1-IN-3 (Compound 1), an APE1 inhibitor, is utilized in cancer research.</p>

<p>2-Acetyl-2-decarboxamidotetracycline is a tetracycline-class antibiotic. It exhibits a UV absorption spectrum similar to that of tetracycline or 5-oxytetracycline at concentrations above 300 mμ, characteristic of the BCD ring system.</p>

<p>Etofamide, an antimicrobial agent, exhibits an IC50 of 5.96 mg/L against amoebae.</p>

<p>Saptomycin E is an antitumor antibiotic.</p>

<p>Kikumycin A, an antibiotic produced by Streptomyces, exhibits antimicrobial activity against both Gram-positive and Gram-negative bacteria. Additionally, it demonstrates antitrichomonal activity with a minimum inhibitory concentration (MIC) of 25 μg/mL against Trichomonas foetus.</p>

<p>GTSE1-IN-1 (compound Y18), an orally active GTSE1 inhibitor, exhibits notable anticancer properties. It effectively represses the proliferation of cancer cells by downregulating GTSE1 transcription and expression, which leads to DNA damage and promotes persistent cell cycle arrest and cellular senescence. Moreover, GTSE1-IN-1 substantially reduces the adhesion, migration, and invasion of colorectal cancer HCT116 cells and non-small cell lung cancer A549 cells in vitro.</p>

<p>17,17-Ethylendioxyandrost-5-en-3β-ol, with an EC 50 of 629 μM, acts as an inhibitor of HSV-1. This compound is applicable in research studies focusing on viral infections.</p>

<p>HBV-IN-48, an HBV inhibitor, exhibits potent antiviral activity against HBV in HepDE19 cells, demonstrated by its EC 50 value of 0.005 μM. Additionally, it effectively reduces serum HBV DNA levels in mouse models of HBV infection.</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>PLpro-IN-6 (compound 6) serves as an inhibitor for the papain-like protease (PLpro), demonstrating potent activity with an IC 50 of 0.019 μM against the SARS-CoV-2 PLpro enzyme.</p>

<p>GC373, an effective inhibitor of the SARS-CoV-2 M pro, impedes virus replication, exhibiting an inhibition concentration (IC 50) of 0.4 μM. This compound is valuable for use in anti-COVID-19 research.</p>

<p>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.</p>

<p>Triazophos is a non-systemic pesticide that acts as an acetylcholinesterase (AChE) inhibitor, forming a covalent and irreversible bond with the acetylcholine binding site. This action blocks the hydrolysis of acetylcholine, leading to increased excitability. It is effective against a wide range of soil insects and mites, including aphids, thrips, midges, beetles, lepidopteran larvae, mole crickets, and red spiders. Triazophos is suitable for use on various crops such as ornamental plants, cotton, rice, corn, soybeans, oil palm, olives, and coffee.</p>

<p>LN002 is an orally active inhibitor of Cryptosporidium oxidase, utilized for research in cryptosporidiosis.</p>

<p>DL-2-Aminopimelic Acid acts as a weak agonist for glutamate receptors and also reduces the sensitivity of leech glutamate receptors to glutamate.</p>

<p>UNI418 is a dual inhibitor targeting PIKfyve and PIP5K1C, exhibiting antiviral activity against SARS-CoV-2 (EC50=1.4 μM). It inhibits the endocytosis of the virus mediated by ACE2 by suppressing PIP5K1C (IC50=60.1 nM; Kd=61 nM). Additionally, UNI418 impedes the entry of SARS-CoV-2 into host cells by inhibiting the proteolytic activation regulated by PIKfyve (Kd=0.78 nM).</p>

<p>MK-8876 is an Inhibitor of HCV NS5B Site D.</p>

<p>LN-439A (compound LN-439A) is a novel BAP1 inhibitor that suppresses the growth of basal-like breast cancer by degrading KLF5.</p>

<p>Arterolane, an adenosine triphosphatase inhibitor, is used potentially for the treatment of malaria.</p>

<p>Inactive enantiomer of Sofosbuvir, used for chronic hepatitis C; lacks reported biological activity.</p>

<p>Isopyrazam, a plant protection product, exhibits potent antifungal activity. When applied to crops, it effectively inhibits the growth of various plant pathogenic fungi, significantly enhancing both the yield and quality of the crops. This compound demonstrates exceptional disease resistance capabilities in agricultural applications.</p>

<p>Lentiginosine is a selective amyloglucosidase inhibitor.</p>

<p>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.</p>

<p>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.</p>

<p>PLpro-IN-5 (compound 21), serving as a PLPro protease inhibitor, boasts an IC50 of 91.14 nM. This compound exhibits a broad-spectrum antivirus efficacy, particularly effective against SARS-CoV, MERS-CoV, and SARS-CoV-2.</p>

<p>MT0703 is a cephalosporin antibiotic featuring an aminothiazolylglycyl moiety with a 1,5-dihydroxy-4-pyridinone-2-carbonyl group, displaying potent activity against Pseudomonas species.</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>AB25583 is a small molecule inhibitor of Polθ helicase (Polθ-hel) with an IC50 of 6 nM. It selectively kills cells deficient in BRCA1/2 and synergizes with Olaparib in cancer cells harboring pathogenic BRCA1/2 mutations. AB25583 can be utilized in tumor research.</p>

<p>Glasmacinal is a non-antibacterial macrolide compound with anti-inflammatory activities.</p>

<p>Streptothricin F is a biochemical.</p>

<p>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.</p>

<p>A 76889 is an inhibitor of HIV-1 protease.</p>

<p>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.</p>

<p>HldA/E-IN-1 (compound 8) is a dual inhibitor of HldA/E, exhibiting IC50 values of 17.2 μM and 67.8 μM, respectively. This compound is utilized in research on antibacterial infections.</p>

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

<p>SARS-CoV-2-IN-99 (compound 58) is an inhibitor of the main protease of SARS-CoV-2.</p>

<p>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.</p>

<p>5-Methylcytosine hydrochloride plays a critical role in regulating gene expression, promoting genomic imprinting, and inhibiting transposon factors. It is also closely associated with translation fidelity and tRNA recognition.</p>

<p>Lamivudine, a drug for HIV-1 and HBV, inhibits reverse transcriptase and resembles zalcitabine.</p>

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

<p>Ambelline has antitumor activity.</p>

<p>GR 122222X is an inhibitor of topoisomerase II.</p>

<p>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.</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>

<p>7-APRA is a semisynthetic intermediate of the cephalosporin class of antibiotics. It exhibits antibacterial activity and is primarily used in the synthesis of other cephalosporin antibiotics, such as Cefaclor and Cefprozil.</p>