Microbiologie/Virologie

<p>Antibacterial Agent 154 (Compound 7), a Fluoroquinolone derivative, exhibits broad-spectrum efficacy against both Gram-positive and Gram-negative bacteria when</p>

<p>Balapiravir HCl, an NS5B inhibitor, is used potentially for the treatment of HCV infection.</p>

<p>12R-LOX-IN-1 (Compound 4a), with an IC50 of 28.25 µM, is an inhibitor of 12R-LOX.</p>

<p>Antifungal agent 49 (Example 112) exhibits activity against Cryptococcus neoformans, demonstrating a minimum inhibitory concentration (MIC) of 49 μM [1].</p>

<p>Antituberculosis agent-8: MIC 3.53 μM vs M. tuberculosis, antifungal MIC 62.50 μM vs A. niger.</p>

<p>Δ2-transEicosenoic acid, an α,β-unsaturated fatty acid, emerges as a by-product during the synthesis of Δ2-ciseicosenoic acid, which along with its salts, shows promise in diabetes treatment and lipid metabolism enhancement. Additionally, the compound 2-octadecenoic acid is recognized for its ability to enhance liver function and reduce blood sugar levels in streptozocin-induced diabetic rats.</p>

<p>Clazuril, a phenylacetonitrile derivative, treats coccidiosis in poultry by killing Eimeria species.</p>

<p>NK007 is a novel anti-SARS-CoV-2 agent with an EC 50 value of 30 nM.</p>

<p>NSC309401 is an E. coli dihydrofolate reductase inhibitor, displaying potency with an IC50 value of 189 nM and a dissociation constant (KD) of 14.57 nM [1].</p>

<p>Antibacterial agent 93: potent aaRS inhibitor; effective against certain gram-positive and negative bacteria.</p>

<p>N-(3-Oxobutanoyl)-L-homoserine lactone (3-oxo-C4-HSL) serves as an autoregulator for carbapenem antibiotic biosynthesis in Erwinia carotovora ATCC 39048 and induces the expression of rhiI in R. leguminosarum [1].</p>

<p>Emzadirib (RAD51-IN-2) is a potent RAD51 inhibitor with potential anticancer activity for the study of DNA damage repair.</p>

<p>Antimalarial agent 15 halts Plasmodium falciparum growth with a 20 nM IC50.</p>

<p>DuP-721: broad-spectrum, oral antibiotic targeting various bacteria, including M. tuberculosis.</p>

<p>SPR38: SARS-CoV-2 protease inhibitor with Ki 0.260 μM; also blocks hCatL (Ki 1.92 μM) and hCatB (Ki 11.1 μM).</p>

<p>Anti-MRSA Agent 8 (Compound 7g), a derivative of DAPG, exhibits potent antibacterial properties by interacting with bacterial cell membranes and is useful for</p>

<p>Beclabuvir (BMS-791325) is an HCV inhibitor targeting NS5B polymerase with sub-28 nM potency for genotypes 1, 3, 4, 5.</p>

<p>Diazoketone methotrexate is an analog of methotrexate with potential antitumor activity.</p>

<p>Isotianil is a plant defense inducer that activates typical plant defense responses without direct antimicrobial effects, serving as a plant protection agent</p>

<p>Limocrocin is an inhibitor of reverse transcriptase.</p>

<p>5,6,7,8-Tetrahydro-8-deazahomofolic acid is a potential thymidylate synthase (TS) inhibitor and other folate related enzymes inhibitor.</p>

<p>Antibiofilm Agent-2 (Compound 4T) serves as a potent biofilm inhibitor, exhibiting an IC50 of 3.6 μM, and impairs the quorum sensing system along with iron</p>

<p>Zndm19 is an inhibitor of New Delhi Metallo-β-lactamase-1 (NDM-1), utilized in researching drug-resistant bacterial infections [1].</p>

<p>Azaconazole, an agricultural fungicide, is used for controlling powdery mildew on crops and bean rust.</p>

<p>TAS-114 is a dUTPase and DPD inhibitor that modulates catabolic pathways to improve systemic availability of 5-FU.</p>

<p>Laxifloran possesses antibacterial and antifungal properties.</p>

<p>NIK-250 is a P-glycoprotein inhibitor. NIK250 could reverse multidrug resistance in human glioma cells.</p>

<p>VT-1598 is a novel, selective, orally active fungal CYP51 inhibitor. VT-1598 exhibits antifungal effects against Candida albicans.</p>

<p>Tuberculosis inhibitor 6 (compound 2c), a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative, is highly active against Mycobacterium tuberculosis (MIC 90 of</p>

<p>APX001 is a prodrug of APX-001A. APX001 is the first-in-class inhibitor of the fungal protein Gwt1.</p>

<p>Antibiofilm Agent-1, as detailed in WO2017011725A1 (compound 17) [1], serves as an antibacterial agent effective against Gram-positive pathogens.</p>

<p>WRN Inhibitor 4 (Example 107), a cyclic vinyl sulfone-based compound, serves as an inhibitor of the Werner Syndrome ATP-dependent helicase enzyme (WRN).</p>

<p>WRN Inhibitor 3 (example 110), a cyclic vinyl sulfone-based compound, serves as an inhibitor of the Werner Syndrome ATP-dependent helicase enzyme (WRN).</p>

<p>UNC-2170 (UNC2170 Maleate) is the methyl-lysine binding protein, 53BP1 ligand.</p>

<p>SARS-CoV-2 3CLpro-IN-2 is a potent inhibitor of the 3CL protease pair and has shown research potential for SARS-CoV-2 disease.</p>

<p>Hinokinin (Cubebinolide), a bioactive lignan, exhibits a broad spectrum of pharmacological activities.</p>

<p>Mtb-IN-4 (compound 17h) is a non-toxic isoxazole that exhibits anti-Mycobacterium tuberculosis (Mtb) activity, with an IC50 value of 0.70 μM.</p>

<p>Daldinone A (Compound 4), isolated from Nigrospora oryzae, exhibits antibacterial properties, specifically demonstrating antimicrobial potential against P. aeruginosa [1].</p>

<p>9-Deazaguanine is a nucleoside analogue exhibiting inhibitory activity against bovine purine nucleoside phosphorylase (PNP).</p>

<p>Antiviral agent 35 (compound 4d) serves as a potent orally active inhibitor of the influenza virus, targeting early stages of viral replication.</p>

<p>6-Chloro-7-deazapurine-β-D-riboside shows antifungal activity.</p>

<p>Valnemulin, a broad-spectrum pleuromutilin antibiotic, targets peptidyl transferase within the 50S ribosomal subunit, effectively used in veterinary medicine to address swine diseases such as B. hyodysenteriae and M. hyopneumoniae.</p>

<p>Antifungal agent 66 (compound 10) exhibits broad-spectrum antifungal activity against seven phytopathogenic fungal mycelia and significant inhibitory effects on</p>

<p>Antibacterial Agent 135 (example 7) effectively inhibits various bacteria, including P.</p>

<p>MAC13772 is a potent inhibitor of the enzyme BioA with an IC50 of 250 nM thereby inhibiting biotin biosynthesis. MAC13772 exhibits antibacterial activity.</p>

<p>DMA-IN-1 is a DNA adenine methyltransferase (DAM) inhibitor with an IC50 value of 48 μM.</p>

<p>4'-Acetyl-chrysomycin B, a 4'-acetylated analog of chrysomycin B, exhibits anti-Gram-positive bacterial and antimicrobial activities [1].</p>

<p>SDH-IN-3 is a succinate dehydrogenase (SDH) inhibitor, demonstrating potent antifungal activity with an inhibition concentration (IC50) of 7.2 μg/mL and an</p>

<p>XSJ2-46, a 5'-amino NI analog, is an antiviral agent possessing anti-Zika virus properties and demonstrates reasonable inhibition of RNA-dependent RNA</p>

<p>RSV L-protein-IN-3 is an inhibitor of the wild-type RSV polymerase, exhibiting an IC50 of 10.4 μM and an EC50 of 2.1 μM (against RSV), and possesses lower</p>

<p>RSV L-protein-IN-5 (Compound E) serves as a potent inhibitor of the Respiratory Syncytial Virus (RSV), with an EC50 value of 0.1 μM.</p>

<p>Oxynitidine, an HBV inhibitor (ID50 = 30.8 µg/mL), effectively suppresses HBV DNA replication and may be utilized in viral infection research [1].</p>

<p>Disoxaril (BRN 3626820, WIN 51711), an anti-picornavirus, blocks enterovirus by targeting VP1; boosts poliovirus inhibition with Ambioxime, Bioxazole.</p>

<p>L 694746 is an inhibitor of HIV-1 protease.</p>

<p>AU1235 is a Mycobacterium tuberculosis inhibitor.</p>

<p>Pyrethrin II, an active insecticidal component of pyrethrins, is a biogenic insecticide derived from Chrysanthemum cinerariifolium [1].</p>

<p>HCoV-OC43-IN-1 (Compound IV-16) serves as an inhibitor of the coronavirus HCoV-OC43, exhibiting antiviral efficacy with an EC50 of 90 nM.</p>

<p>SARS-CoV-2 3CLpro-IN-15 (compound a), a beta-nitrostyrene derivative, acts as an inhibitor of the SARS-CoV-2 3CL protease (3CLpro), effectively inhibiting viral</p>

<p>NSC 288387, a pan-flavivirus MTase inhibitor, binds to the SAM-binding pocket and effectively inhibits Zika virus (ZIKV) with an IC50 of 0.2 μM, also preventing</p>

<p>RSV L-protein-IN-2 (Compound A), a noncompetitive inhibitor of the RSV polymerase (IC50: 4.5 μM), exhibits antiviral activity against long RSV strains (EC50: 1.</p>

<p>Votoplam functions as a gene splicing modulator, employed in the inhibition of Huntington's disease [1].</p>

<p>NS5A-IN-2, a potent inhibitor, is highly effective against HCV 1b and shows increased activity for GT 3a with good metabolic stability.</p>

<p>ZINC475239213 acts as an inhibitor targeting the SARS-CoV-2 Nsp14 N7-Methyltransferase with an IC50 value of 20 μM [1].</p>

<p>Antileishmanial agent-17, a coumarin hybrid, exhibits potent antileishmanial activity (IC50 &lt;0.78 μM) while proving non-toxic to normal VERO cells.</p>

<p>N,O-Diacetyltyramine, isolated from the actinomycete Pseudonocardia endophytica VUK-10, exhibits both antibacterial activity against Gram-positive and Gram-negative bacteria, alongside fungi, and demonstrates cytotoxicity towards MDA-MB-231, HeLa, MCF-7, and OAW-42 cells [1].</p>

<p>Urease-IN-6, a potent Urease inhibitor, exhibits an IC50 value of 14.2 μM and is utilized in the research of peptic and gastric ulcers [1].</p>

<p>WRN Inhibitor 5 (Example 157), a cyclic vinyl sulfone-based compound, serves as an inhibitor of Werner Syndrome ATP-dependent helicase enzyme (WRN).</p>

<p>BVDU 5′-Triphosphate is an antiviral agent labeled with 5′-Triphosphate that specifically targets viral DNA polymerase.</p>

<p>Arbemnifosbuvir, a drug interfering with the nidovirus DdRp-associated nucleotidyltransferase (NiRAN) domain of non-structural protein 12 (nsp12), is utilized</p>

<p>L 687908 is a potent inhibitor of hydroxyethylene-containing HIV protease.</p>

<p>MPI8 is a SARS-CoV-2 Protease inhibitor (IC50 = 105 nM).</p>

<p>HIV-1 integrase inhibitor 3 is an HIV-1 integrase strand transfer (INST) inhibitor (IC50: 2.7 nM).</p>

<p>Phenethicillin sodium (α-Phenoxyethylpenicillin) is a penicillin-class antibiotic that exhibits antimicrobial activity [1].</p>

<p>NVS-SM2 boosts SMN2 splicing, enhances exon 7 inclusion, and raises SMN protein levels orally.</p>

<p>Vaborbactam (RPX7009) is a β-lactamase inhibitor that is often used in conjunction with meropenem to study pneumonia and CRE infections.</p>

R 87366 is used as a water-soluble HIV protease inhibitor.

<p>HBV-IN-12 is a potent inhibitor of hepatitis B surface antigen (HBsAg).</p>

<p>HBV-IN-30, a flavone derivative, inhibits cccDNA in HBV research.</p>

<p>SARS-CoV-2/MERS Mpro-IN-2 is a potent inhibitor of the main proteases of SARS-CoV-2 and MERS, demonstrating IC50 values of 0.21 and 0.07 µM, respectively.</p>

<p>L-742001 Hydrochloride is an RNA polymerase inhibitor.</p>

<p>S-Adenosylhomocysteine (SAH) hydrolase is responsible for the reversible hydrolysis of SAH into adenosine and homocysteine. Inhibition of this enzyme leads to the accumulation of SAH within cells, thereby increasing the SAH to S-adenosylmethionine (SAM) ratio and subsequently inhibiting SAM-dependent methyltransferases. (−)-Neplanocin A, a potent and irreversible inhibitor of SAH hydrolase (Ki= 8.39 nM), exhibits significant antitumor activity against mouse leukemia L1210 cells and holds broad-spectrum antiviral properties. Its efficacy notably surpasses that of the reversible inhibitor 3-deazaneplanocin, especially in combating vesicular stomatitis, evidencing a higher potency with ID50 values of 0.07 μg/ml for Neplanocin A versus 0.3 μg/ml for 3-deazaneplanocin.</p>

<p>Yimitasvir diphosphate, also known as Emitasvir, is an orally-administered inhibitor of the hepatitis C virus (HCV) nonstructural protein 5A (NS5A).</p>

<p>Mpro 61 is a potent non-covalent inhibitor of SARS-CoV-2 main protease.</p>

<p>Annamycin, a semi-synthetic doxorubicin derivative, binds DNA, blocks topoisomerase II, and evades MDR, inhibiting DNA/RNA/protein synthesis.</p>

<p>Kynostatin-272 is a HIV protease inhibitor. KNI-272 blocked the maturation of viral particles.</p>

<p>BMS-561390, a reverse transcriptase inhibitor, is used potentially for the treatment of HIV infection.</p>

<p>CcpA-IN-1 is a Staphylococcus aureus antibiotic exhibiting significant bactericidal activity (MICs=460 nM) [1].</p>

<p>SARS-CoV-2-IN-1 is a potent inhibitor of Mpro(SARS-CoV-2 Mpro, SARS-CoV Mpro and MERS-CoV Mpro with IC50s of 0.67, 0.90 and 0.58 μM, respectively).</p>

<p>AZD-7295 (A-689) is an NS5A inhibitor that may be used to treat HCV infection.</p>

<p>Ganfeborole HCl (GSK3036656 HCl) is a compound with anti-tuberculosis activity and is an inhibitor of Mycobacterium tuberculosis (Mtb) leucyl-tRNA synthetase.</p>

<p>Besifovir Dipivoxil maleate, an oral HBV prodrug (LB80380), suppresses HBV DNA in naive and lamivudine-resistant CHB cases.</p>

<p>Dihydroaltenuene B inhibits mushroom tyrosinase (IC50: 38.33µM) and binds His244, Met280, Gly281 via hydrogen bonds.</p>

<p>Mansonone F is a topoisomerase II inhibitor with cytotoxic and topo inhibitory potencies.</p>

<p>Antifungal agent 77 (Compound 13h) exhibits not only antifungal properties, but also effective insecticidal activity against Mythimna separata, Helicoverpa</p>

Levofuraltadone is an antiprotozoal and antibacterial agent.

<p>Zevotrelvir (Compound 52) serves as an inhibitor of coronavirus, demonstrating IC50 values below 0.1 μM for 229E hCoV protease and below 0.1 mM for SARS-CoV-3C-</p>

<p>Lagociclovir valactate is a prodrug of Lagociclovir . Lagociclovir valactate is an orally active anti- HBV agent [1] .</p>

<p>WRNA10 is a potent binding agent for HIV-1TAR RNA (IC50: 10 μM, CC50: 40 μM).</p>

<p>Compound 17b, an amino alcohol-quinoline, targets Pf3D7 (IC50: 14.9 nM) and PfW2 (IC50: 11 nM) with selectivity index &gt;770.</p>

<p>Cyclopropavir (Filociclovir; MBX-400) is a broad-spectrum anti-herpes drug effective against CMV and HHV-6/8 (EC50: 0.7-8 μM).</p>