Microbiology/Virology

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

<p>Levofuraltadone is an antiprotozoal and antibacterial agent.</p>

<p>SARS-CoV-2-IN-59 (compound E07), an imidazoline derivative, is a non-peptide small molecule that inhibits SARS-CoV-2 by targeting its main protease (Mpro).</p>

<p>H3B-968 is a potent inhibitor of Werner syndrome protein (WRN) with an IC50 of approximately 10 nM, effectively targeting its helicase, ATPase, and exonuclease</p>

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

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

<p>Pinokalant (LOE-908) is a novel non-selective cation channel inhibitor.Pinokalant significantly reduces cortical infarct volume in in vivo experiments, improves</p>

<p>DMP 323 is a potent inhibitor of HIV-1 protease.</p>

<p>SLU-10482, an antiparasitic agent, effectively reduces C.</p>

<p>Prochloraz manganese, an antifungal agent utilized in the agricultural sectors [1], serves to protect crops by inhibiting fungal growth.</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>NSC309401 is an E. coli dihydrofolate reductase inhibitor with an IC50 value of 189 nM and a dissociation constant (Kd) of 14.57 nM [1].</p>

<p>1,8-Dichloroanthraquinone, a derivative of anthraquinone, effectively inhibits sulfide production in sulfate-reducing bacteria [1].</p>

<p>Flurofamide is an effective bacterial urease inhibitor and has potential in the treatment of infected urinary calculi.</p>

<p>Compound 158 (6c), a Micrococcin analogue, serves as an antibacterial agent effective against impetigo and Clostridium difficile infection (CDI) [1].</p>

<p>Tuberculosis inhibitor 7 (compound 2d), a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative, exhibits potent activity against Mycobacterium tuberculosis and</p>

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

<p>7-Deaza-2',3'-dideoxyguanosine (7-Deaza-ddG) is a 2′,3′-dideoxynucleoside 5′-triphosphate that inhibits HIV-1 reverse transcriptase with a Ki of 25 nM [1].</p>

<p>GSK3532795: potent oral HIV-1 maturation inhibitor; EC50: 1.9-13 nM for various strains.</p>

<p>Antiviral agent 43 (compound 16) serves as a potent, orally active inhibitor of influenza A virus entry, demonstrating efficacy by inhibiting the replication of the influenza A strains VH04-H5N1 and PR8-H1N1 with EC50 values of 240 nM and 72 nM, respectively [1].</p>

<p>17(R)-Resolvin D4 (17(R)-RvD4) is an epimer of RvD4, generated through the aspirin-induced modification process.</p>

<p>RAD51-IN-4, a potent RAD51 inhibitor, may be useful in researching mitochondrial defect-related conditions.</p>

<p>Pen is an oral cancer drug that blocks DNA synthesis by inhibiting key enzymes and integrating into DNA.</p>

<p>HBV-IN-41 (compound 45) is a potent, orally active inhibitor of Hepatitis B Virus (HBV), exhibiting an EC50 value of 0.027μM [1].</p>

<p>β-Lactamase-IN-8 (compound 20) is a potent and oral bioavailable broad-spectrum cyclic boronate β-lactamase inhibitor that can be used for researching</p>

<p>L-696229: specific HIV-1 RT inhibitor, blocks viral spread in various cells.</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>Y18501, an oxysterol-binding protein (OSBPI) inhibitor structurally akin to Oxathiapiprolin, demonstrates potent inhibition against Phytophthora spp.</p>

<p>HEC72702: New HBV capsid inhibitor, from GLS4. No CYP1A2, CYP3A4, CYP2B6 induction at 10μM.</p>

<p>Antibacterial compound 2 is a potent antimicrobial agent effective against many human veterinary pathogens, inhibiting multi-drug resistant staphylococci,</p>

<p>Tirapiravir is an antiviral nucleoside analog that exhibits activity against both the novel coronavirus and influenza virus [1].</p>

<p>FIKK9.1-IN-1 (Compound 1), an antimalarial agent (IC50: 2.68 μg/mL), serves as a FIKK9.1 inhibitor by interacting with the ATP-binding residues within FIKK9.1,</p>

<p>JTK-853: novel non-nucleoside HCV polymerase inhibitor with strong antiviral activity (EC50: 0.38 μM genotype 1a, 0.035 μM 1b).</p>

<p>AZ-27 is a respiratory syncytial virus inhibitor which differentially inhibits different polymerase activities at the promoter.</p>

<p>Nilofabicin (CG-400549) is a potent inhibitor of enoyl-(acyl-carrier-protein) reductase fall(FabI) and can be used in studies about the treatment of complicated</p>

<p>Aminoacyl tRNA synthetase-IN-1 is an inhibitor of bacterial aminoacyl tRNA synthetase (aaRS).</p>

<p>ThrRS-IN-3: Potent inhibitor of Salmonella enterica ThrRS, IC50 = 19 nM, Kd = 34 nM, with antibacterial effects.</p>

<p>Caerulomycin A (Caerulomycin) (Cerulomycin; Caerulomycin) is an antifungal compound.</p>

<p>Chitin Synthase Inhibitor 14 (compound 4n), a potent chitin synthase (CHS) inhibitor, exhibits antifungal activity and is effective against drug-resistant</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>DNA polymerase-IN-3 (Compd 5b), a coumarin derivative, demonstrates inhibitory activity against Taq DNA polymerase and has potential applications in</p>

<p>Phylloflavan, an antileishmanial compound, exhibits an intracellular half maximal effective concentration (EC50) of 3.2 nM in RAW 264.7 cells and inhibits the</p>

<p>Amoxicillin-clavulanate potassium is an orally administered antibiotic and combination agent indicated for various bacterial infections.</p>

<p>Zika virus-IN-2 (Compd 3) is a Zika virus inhibitor (EC 50= 7.4 μM).</p>

<p>3β-Hydroxy-hop-22(29)-ene is a potent antiparasitic compound demonstrating moderate efficacy against Trypanosoma cruzi and Leishmania mexicana.</p>

<p>Murabutide, a safe synthetic immunomodulator, diminishes the expression of CD4 and CCR5 receptors and promotes the secretion of high levels of beta-chemokines,</p>

<p>HCV-IN-44 (compound 28) is an inhibitor of the HCV NS5B protein, efficacious in suppressing HCV virus replication and useful for researching HCV infection [1].</p>

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

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

<p>Roseoflavin, a chemical analog of FMN and riboflavin that has antimicrobial activity, can directly bind to FMN riboswitch aptamers and downregulate the</p>

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

<p>DHFR-IN-10 (compound 4c) is a potent inhibitor of dihydrofolate reductase (DHFR), displaying an inhibition concentration half-maximum (IC50) of 4.21 μM against</p>

<p>Tobevibart, an IgG1-lambda humanized monoclonal antibody targeting the hepatitis B virus (HBV) surface envelope protein, exhibits antiviral activity [1].</p>

<p>1R-cis-Permethrin, an insecticide and neurotoxin, acts on neuron membranes by extending the activation of sodium channels [1].</p>

<p>DQn-1, a potent antifolate, demonstrates efficacy against Mycobacterium tuberculosis (Mtb) with an MIC 90 of 0.03 µM.</p>

<p>Fosalvudine tidoxil, a nucleoside reverse transcriptase inhibitor, is used potentially for the treatment of HIV infection.</p>

<p>Tuberculosis Inhibitor 12, an oxadiazole derivative, effectively inhibits Mycobacterium tuberculosis, demonstrating inhibition rates of 82% and 78% at a</p>

<p>Compound 5b, an antibacterial, effectively targets MRSA and disrupts bacterial membranes and PG synthesis.</p>

<p>ELQ-596, a quinolone derivative, exhibits antimicrobial activity against several protozoan parasites, including the intraerythrocytic parasites Plasmodium and Babesia. ELQ-596 attenuates babesiosis in immunosuppressed mice [1].</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>NS5A-IN-3 is a potent NS5A inhibitor with high efficacy against HCV 1b, good activity on 3a, and strong metabolic stability; superior to daclatasvir.</p>

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

<p>Berkeleylactone E, a macrolide antibiotic [1], exhibits antimicrobial properties.</p>

<p>FR194738 free base inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC50 of 9.8 nM. </p>

<p>UCB7362 (GLXC-26743) is an orally available and potent plasmepsin X (PMX) inhibitor with anti-malarial activity.UCB7362 inhibits parasite reproduction.</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>Deacylketoconazole (Deacyl ketoconazole) is a Ketoconazole derivative and is also an antifungal agent.</p>

<p>Antibacterial compound 1 is an antibacterial compound.</p>

<p>TH-Z145 is a potent FPPS inhibitor for the study of myeloma and lung cancer.</p>

<p>MsbA-IN-6: potent antibiotic, hinders MsbA in gram-negative bacteria, kills E. coli, effective on drug-resistant strains.</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>IpOHA is a potent inhibitor of plant KARI and functions as an antimycobacterial agent, demonstrating a K_i value of 97.7 nM against Mycobacterium tuberculosis (</p>

<p>DDD85646 is an inhibitor of T. brucei N-myristoyltransferase with a Ki of 1.44 nM, an IC50 of 2 nM and an EC50 of 2 nM. The IC50 of hNMT is 4 nM.</p>

<p>PTC725 is a selective HCV 1b replicons inhibitor. It has been shown to target the nonstructural protein 4B.</p>

<p>A 77003 is a HIV-1 protease inhibitor. A77003 impairs HIV-1 protease-mediated Gag processing.</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>L 694746 is an inhibitor of HIV-1 protease.</p>

<p>ISPA-28: reversible PSAC antagonist via direct CLAG3 binding.</p>

<p>HIV-1 inhibitor-3 is an HIV infection inhibitor.</p>

Icofungipen is an oral antifungals with active against Candida species.

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

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

<p>Kynostatin-272 is a HIV protease inhibitor. KNI-272 blocked the maturation of viral particles.</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>NCI-B16 is a small-molecule RNA binder that inhibits HCV (hepatitis C virus) replication [1].</p>

<p>5,11-methenyltetrahydrohomofolate blocks GAR &amp; AIR transformylase; used as an anti-purine drug.</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>Pexiganan acetate (MSI 78), a 22-residue peptide analogue of magainin 2, disrupts bacterial membranes or walls, leading to antibacterial activity.</p>

<p>U 89360E is a peptidic inhibitor.</p>

<p>A 74704 is a pseudo C2-symmetric inhibitor of HIV-1 protease and its diester analog.</p>

<p>Bio-AMS is a potent inhibitor of bacterial biotin protein ligase, exhibiting selective activity against Mycobacterium tuberculosis (Mtb) and disrupting fatty</p>

<p>T145 halts key bacteria growth at sub μg/ml, deters resistance, and may enhance drug lifespan.</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>

<p>(E)-LHF-535, an E-isomer antiviral, EC50 &lt;1 μM vs Lassa/Machupo/Junin, 1-10 μM vs VSVg.</p>

<p>Propiolactone (β-propiolactone; 2-Oxetanone), a chemosterilant, effectively inactivates viruses, rendering them non-infectious.</p>

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<p>Fenpropidin (Ro-12-3049), a fungicide, is a specific inhibitor of sterol 14-reductase and biosynthesis.</p>