Microbiology/Virology

<p>Zika virus-IN-1 is an inhibitor of Zika virus (EC50: 1.56 μM).</p>

<p>DGKα-IN-8 (Example 51) is a potent diacylglycerol kinase alpha (DGKα) inhibitor, exhibiting an IC50 of 22.491 nM and an EC50 of 0.256 nM.</p>

<p>4-Aminosalicylic acid hemicalcium, an orally active antibiotic, shows potential in tuberculosis research [1].</p>

<p>Ianthelliformisamine B TFA, an antibiotic enhancer, is used to against resistant Gram-negative bacteria.</p>

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

<p>Deacylketoconazole (Deacyl ketoconazole) is a Ketoconazole derivative and is also an antifungal agent.</p>

<p>A 33853 is an antibiotic isolated from culture broth of Streptomyces sp.</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>XZ426 is a potent integrase strand transfer inhibitor with anti- HIV activity .</p>

<p>BMS-433771 dihydrochloride hydrate is a potent oral RSV inhibitor, affects groups A &amp; B, with a 20 nM EC50, used in respiratory disease research.</p>

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

<p>AB-836, an orally active hepatitis B virus (HBV) capsid inhibitor, hampers viral replication by engaging with the HBV core protein.</p>

<p>BDM91270 (compound 29) serves as an inhibitor of the E.</p>

<p>ddUTP (2′,3′-Dideoxyuridine-5′-triphosphate) serves as a selective inhibitor of HIV and AMV reverse transcriptases with Ki values of 0.05 µM for HIV and 1 µM</p>

<p>GSK-2485852, a NS5B inhibitor, is used potentially for treatment of HCV infection.</p>

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

<p>Compound 5k (Antiproliferative Agent-18) is an antiproliferative agent that exhibits moderate antibacterial and antifungal activities [1].</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>L-697661, a reverse transcriptase inhibitor, is used potentially for the treatment of HIV infection.</p>

<p>SARS-CoV-2 Mpro-IN-12 (compound D026) serves as an inhibitor of the main protease (Mpro) of SARS-CoV-2, exhibiting antiviral properties [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>D1N52 is a potent inhibitor of the SARS-CoV-2 3CL protease, demonstrating an inhibitory concentration half-maximal (IC50) value of 0.53 μM [1].</p>

<p>SARS-CoV-2 3CLpro-IN-5 is a covalent inhibitor targeting the 3C-like protease (3CLpro), exhibiting potent inhibitory activity with an IC50 of 3.8 nM and</p>

<p>Antileishmanial agent-16 (compound 14c), an anti-Leishmania agent, exhibits potent activity against Leishmania major promastigotes (IC50 = 0.59 µM) and</p>

<p>DHX9-IN-4 is an ATP-dependent RNA helicase DHX9 inhibitor used in cancer research.</p>

<p>Oxamniquine is an effective compound for the treatment of schistosomiasis.</p>

<p>Antifungal agent 48 (Example 308), active against Cryptococcus neoformans, exhibits a minimum inhibitory concentration (MIC) value of 11 μM [1].</p>

<p>NNRTIs-IN-1 is a potent non-nucleoside reverse transcriptase inhibitor (NNRTI) with notable anti-resistance efficacy, effectively inhibiting both the wild-type</p>

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

<p>YH-53: potent inhibitor for SARS-CoV-1 (Ki=6.3 nM) &amp; SARS-CoV-2 3CLpro (Ki=34.7 nM); hinders SARS-CoV-2 replication; aids COVID-19 research.</p>

<p>Pen is an oral cancer drug that blocks DNA synthesis by inhibiting key enzymes and integrating into DNA.</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>Besifovir Dipivoxil maleate, an oral HBV prodrug (LB80380), suppresses HBV DNA in naive and lamivudine-resistant CHB cases.</p>

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

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

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

<p>Compound 158 (6c), a Micrococcin analogue, serves as an antibacterial agent effective against impetigo and Clostridium difficile infection (CDI) [1].</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>Antiviral agent 35 (compound 4d) serves as a potent orally active inhibitor of the influenza virus, targeting early stages of viral replication.</p>

<p>LY 173013 is a bicyclic pyrazolidinone, it has antibacterial properties.</p>

<p>GSK3839919A is a potent allosteric inhibitor of HIV-1 integrase [1].</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>Levofuraltadone is an antiprotozoal and antibacterial agent.</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>UNC-2170 (UNC2170 Maleate) is the methyl-lysine binding protein, 53BP1 ligand.</p>

<p>GSK-625433: Homochiral inhibitor blocks HCV genotypes 1a/1b polymerase.</p>

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

<p>MF 5137 is an effective antimicrobial agent.</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>BMS-561390, a reverse transcriptase inhibitor, is used potentially for the treatment of HIV infection.</p>

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

<p>AG 85 is a major secretion protein of Mycobacterium tuberculosis.</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>Pradimicin A derivative 26 exhibits antifungal, antiviral, and antiparasitic properties by attaching to d-mannose (Man)-rich glycans in pathogenic organisms [1</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>β-Lactamase-IN-2 is an inhibitor of β-Lactamase with anti-microbial and anti-bacterial effects.</p>

<p>RSV604 R enantiomer is the R-enantiomer of RSV604. RSV604 is a respiratory syncytial virus (RSV) replication inhibitor.</p>

<p>Ravidasvir, also known as PPI-668 and ASC16, is a second-generation, orally active, potent and selective HCV NS5A protein inhibitor.</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>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>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>CDD-1845, a non-covalent, non-peptide inhibitor, exhibits potent inhibition of SARS-CoV-2 M^pro with a K_i value of 3 nM.</p>

<p>SHR5133 is a potent, orally active regulator of HBV capsid assembly that reduces HBV DNA (EC50: 26.6 nM).</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>Capravirine, a non-nucleoside reverse transcriptase inhibitor, is used potentially for the treatment of HIV infection.</p>

<p>Peptide 46 is a short peptide that inhibits SC-dependent DNA synthesis by targeting the bacterial sliding clamp (SC).</p>

<p>SARS-CoV-2-IN-44, an inhibitor of SARS-CoV-2, effectively suppresses viral replication with an EC50 value of 0.6μM and exhibits negligible cytotoxicity in Calu-</p>

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

<p>LS-BF1: Stable, low-toxic antimicrobial peptide targeting ESKAPE pathogens via cell membrane disruption, effective in mouse infection model.</p>

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

<p>BAY-Y 3118, a new chlorofluoroquinolone, has antimicrobial activity.</p>

<p>Antifungal agent 50 exhibits minimum inhibitory concentrations (MICs) ranging from less than 0.063 to 1 μg/mL [1].</p>

<p>DprE1-IN-9 (compound B18) is an efficient reversible inhibitor of DprE1, interacting with the enzyme's receptor cavity.</p>

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

<p>GS-6620 is a HCV nonstructural protein 5B (NS5B) inhibitor.</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>Anti-Trypanosoma cruzi agent-3 is an antiprotozoal agent.</p>

<p>Acorafloxacin: broad-spectrum fluoroquinolone antibacterial for acute skin infections and pneumonia.</p>

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

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

<p>Methyl 2-amino-5-bromobenzoate (Methyl 5-Bromoanthranilate) is an HCV NS5b RNA polymerase inhibitor with antimicrobial activity.</p>

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

Icofungipen is an oral antifungals with active against Candida species.

<p>ZIKV-IN-1 blocks Zika virus effectively (EC50: 2.8 μM, EC90: 6.8 μM), targets the RdRp domain, and is low-toxic.</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>HIV-1 inhibitor-10 is a nanomolar HIV-1 maturation inhibitor.</p>

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

<p>BMY-43748 is an antibacterial compound with great in vitro and in vivo antibacterial activity.</p>

<p>IR415 selectively interacts with Hepatitis B virus X protein (HBx, Kd = 2 nM) and blocks HBV-mediated RNAi suppression, reverses the inhibitory effect of HBx</p>

<p>Orysastrobin, a "quinone outside inhibitor" (QoI) fungicide, demonstrates outstanding efficacy in controlling rice leaf and panicle blast as well as sheath</p>

<p>U 104489 (PNU-104489) is a novel specific inhibitor of human immunodeficiency virus 1 (HIV-1), showing effective activity against BHA-P-resistant HIV-1MF.</p>

<p>RO-7 is a next-generation polymerase (PA) endonuclease influenza A and B viruses inhibitor.</p>

<p>ST-148 maleate, a potent and orally active DENV inhibitor, exhibits antiviral efficacy with low cell toxicity. It disrupts the interaction between lipid droplets and the C protein, inhibiting viral replication. [1]</p>