Microbiologia/Virologia

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

<p>8-Azahypoxanthine (NSC-22709) inhibits hypoxanthine-guanine-xanthine phosphoribosyltransferase and has antimalarial properties.</p>

<p>Zoxamide (RH-7281) is an oomycete-specific fungicide that impedes nuclear division in Phytophthora capsici germlings and disrupts the microtubule cytoskeleton [</p>

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

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

<p>I-A09 is a noncompetitive mPTPB inhibitor.</p>

BAY-Y 3118, a new chlorofluoroquinolone, has antimicrobial activity.

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

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

<p>BRL44385 is an effective and selective inhibitor of the replication of HSV-1 and HSV2, Epstein-Barr virus (EBV), and varicella-zoster virus (VZV).</p>

<p>DprE1-IN-9 (compound B18) is an efficient reversible inhibitor of DprE1, interacting with the enzyme's receptor cavity.</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>Bio-AMS is a potent inhibitor of bacterial biotin protein ligase, exhibiting selective activity against Mycobacterium tuberculosis (Mtb) and disrupting fatty</p>

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

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

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

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

<p>9-Deazaguanine is a nucleoside analogue exhibiting inhibitory activity against bovine purine nucleoside phosphorylase (PNP).</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>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>Antileishmanial agent-23 (compound G1/9), a potent and selective trypanothione reductase (TR) inhibitor, exhibits an IC50 of 2.24 ± 0.52 μM.</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>TH-Z145 is a potent FPPS inhibitor for the study of myeloma and lung cancer.</p>

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

<p>Antifungal agent 24 (Compound 6) is an antifungal agent that inhibits Candida albicans (MIC: 0.03 μg/ml).</p>

ALS-8112 is a inhibitor of respiratory syncytial virus (RSV) polymerase. The 5'-triphosphate form of ALS-8112 inhibits RSV polymerase (IC50: 0.02 μM).

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

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

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

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

<p>AG 85 is a major secretion protein of Mycobacterium tuberculosis.</p>

<p>RNA polymerase II-IN-1 (19iv), an amatoxin, inhibits Pol II at 36.66 nM IC50, is more toxic to cancer cells, less to normal cells than α-Amanitin.</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>4-Hydroxy-2-methylbenzene ammonium: Policresulen impurity, inhibits NS2B/NS3 protease (IC50: 0.48 μg/mL), hinders DENV2 in BHK-21 cells (IC50: 4.99 μg/mL).</p>

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

Avarofloxacin (JNJ-Q2) is a fluoroquinolone for treating bacterial skin infections and pneumonia.

<p>KY386 is a potent and selective DHX33 helicase inhibitor with an IC50 value of 19 nM.</p>

<p>8-NH2-ATP tetrasodium, an inactive ATP variant, originates from 8-NH2-Ado tetrasodium, which triggers the apoptosis-associated cleavage of poly (ADP-ribose) polymerase [1] [2].</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>Vinclozolin M2, an active metabolite of vinclozolin, is generated through successive esterase activity and decarboxylation in C. elegans, as well as decarboxylation in human liver microsomes. It functions as an antagonist to the mineralocorticoid (IC50= 1,400 nM) and androgen receptors (IC50= 0.17 nM), demonstrated in reporter assays with MCF-7 cells. This compound is exclusively sold for research and analytical purposes, tailored for controlled laboratory use, and is not available in bulk sizes.</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>DuP-721: broad-spectrum, oral antibiotic targeting various bacteria, including M. tuberculosis.</p>

<p>Despropylene gatifloxacin, a metabolite of AM-1155, exhibits potent antibacterial activity and has favorable pharmacokinetics [1].</p>

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

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

DHX9-IN-6 is a highly effective ATP-dependent RNA helicase A (DHX9) inhibitor, used in cancer research.

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

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

<p>Cladosporin, from Cladosporium cladosporioid fungus, halts dermatophyte growth on agar at 75 μg/mL.</p>

<p>Ipflufenoquin, an insecticide, effectively combats primary apple scab infections. Its application is optimal between the stages of half an inch of green and fruit set [1].</p>

<p>2-Dodecanol suppresses both hyphal development and SIR2 gene expression in Candida albicans [1].</p>

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

<p>Emzadirib (RAD51-IN-2) is a potent RAD51 inhibitor with potential anticancer activity for the study of DNA damage repair.</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>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>HBV-IN-12 is a potent inhibitor of hepatitis B surface antigen (HBsAg).</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>Eugenitin, a polyketide from Mycoleptodiscus indicus, exhibits inhibitory activity against Leishmania major with an LD50 of 39.9 μM and demonstrates low</p>

<p>A 33853 is an antibiotic isolated from culture broth of Streptomyces sp.</p>

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

<p>CDD-1819, a non-covalent and non-peptide compound, serves as a potent SARS-CoV-2 Mpro inhibitor, exhibiting a K i value of 5 nM.</p>

<p>Cyclic HPMPC: Potent antiviral, raises O2 in mice with lethal vaccinia, lowers guinea pig CMV replication.</p>

<p>Rosoxacin (Acrosoxacin) shows antibacterial activities against a broad spectrum of Gram-negative bacteria including Neisseria gonorrhoeae (MIC90 = 0.03mg/ml).</p>

<p>Teropavimab (3BNC117-LS), an antibody, is utilized in the research of HIV infection [1].</p>

<p>D1N8 is a potent inhibitor of the SARS-CoV-2 3CL protease, displaying an IC50 value of 0.44 μM and a CC50 value of greater than 20 μM.</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>HEC72702: New HBV capsid inhibitor, from GLS4. No CYP1A2, CYP3A4, CYP2B6 induction at 10μM.</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>Antifungal agent 66 (compound 10) exhibits broad-spectrum antifungal activity against seven phytopathogenic fungal mycelia and significant inhibitory effects on</p>

<p>BILR-355 is a reverse transcriptase inhibitor.</p>

<p>Fervenulin, from Streptomyces sp. CMU-MH021, halts egg hatch (MIC: 30 μg/mL) and kills J2 larvae (MIC: 120 μg/mL) of M. incognita.</p>

<p>3,4'-Dihydroxyflavone (3,4'-DHF) is an oral active flavonoid. 3,4'-Dihydroxyflavone (3,4'-DHF) shows antiviral activity against Influenza A virus.</p>

<p>SIMR3030, a potent inhibitor of SARS-CoV-2 PLpro, possesses an IC50 of 0.0399 µg/mL and demonstrates antiviral activity by diminishing the expression of SARS-</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>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>Du011 is a biogenesis inhibitor of the E.</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>Mpro 61 is a potent non-covalent inhibitor of SARS-CoV-2 main protease.</p>

<p>Streptovitacin A boosts growth inhibition against fungi.</p>

DMP 323 is a potent inhibitor of HIV-1 protease.

<p>Antibiofilm agent-9 (Compound 4), a derivative of pyrrolnitrin, exhibits antimicrobial activity. It inhibits Bacillus anthracis with a Minimum Inhibitory Concentration (MIC) of 0.031 μg/mL. The compound demonstrates significant antibiofilm activity, achieving an inhibition rate of 84% after 24 hours at a concentration of 8.0 μg/mL. Additionally, Antibiofilm agent-9 shows favorable pharmacokinetic properties in mouse models.</p>

<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>hDHODH-IN-1 is an inhibitor of human dihydroorotate dehydrogenase (hDHODH) with an anti-inflammatory effect.</p>

<p>Compound 6d (Antibacterial agent 159) is an antibiotic effective against impetigo and Clostridium difficile infection (CDI), with no observed recurrence for CDI</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>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>NIK-250 is a P-glycoprotein inhibitor. NIK250 could reverse multidrug resistance in human glioma cells.</p>

<p>AVG-233 is an RNA-dependent RNA polymerase (RdRp) inhibitor with antiviral activity for the study of respiratory syncytial virus infections.</p>

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

<p>AS-2077715, an antifungal agent, exhibits inhibitory activity against Trichophyton species and is derived from the fermentation broth of Capnodium sp. 339855. It is utilized in the study of fungal infections [1].</p>

<p>AB131, an inhibitor of MSMEG 6649 and Rv2172c (KD values of 0.16 and 0.02 μM, respectively), enhances the antimycobacterial efficacy of the antitubercular agent</p>

<p>Loflucarban (Fluonilid) is an antimycotic compoud.</p>

<p>Ibuzatrelvir (PF-07817883) is an antiviral compound designed to inhibit the SARS-CoV-2 3CL protease, and is utilized in the treatment of COVID-19 [1].</p>

<p>Ulonivirine is an orally active non-nucleoside reverse transcriptase inhibitor that exhibits high antiviral activity and can be used to study HIV-1 infection.</p>

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

<p>CDD-1733 is a potent, non-covalent, and non-peptide inhibitor of the SARS-CoV-2 main protease (Mpro) with an inhibition constant (K i) of 12 nM.</p>

<p>WRN Inhibitor 2 (example 118), a potent inhibitor of the WRN (Werner Syndrome ATP-dependent helicase enzyme), exhibits a pIC50 value of 7.0 or greater [1].</p>

<p>FAICAR (5-Formamidoimidazole-4-carboxamide ribotide), a purine nucleotide, plays a crucial role in metabolic processes.</p>

<p>SARS-CoV-2/MERS Mpro-IN-1 is a potent inhibitor of the main proteases in SARS-CoV-2 and MERS, exhibiting IC50 values of 0.10 and 0.06 µM, respectively.</p>

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