Microbiologia/Virologia

<p>Trimetozine (Sedoxazine) is a sedative that has been marketed in Europe since 1959. It has mild tranquilizing effects and has been used to treat anxiety.</p>

<p>SARS-CoV-2-IN-13, a stable niclosamide analogue, enhances oral bioavailability and inhibits SARS-CoV-2 (IC50: 0.057 μM).</p>

<p>2'-C-Methyladenosine from C. renalis inhibits HCV, NS5B RNA synthesis (IC50: 0.3, 1.9µM), and LRV1 in L. guyanensis, L. braziliensis.</p>

<p>MProinhibitor 11a: SARS-CoV-2 MPro blocker, IC50=0.053μM; cuts viral yield/RNA in Vero E6 cells, EC50=0.53μM, effective 1.85-50μM.</p>

<p>Besifovir PM (LB80331 PM) is an analogue of Besifovir, a novel orally available acyclic nucleotide phosphonate for the treatment of chronic hepatitis B</p>

<p>Sovaprevir is a non-structural 3 (NS3) protease inhibitor with antiviral activity for the treatment of HCV infection.</p>

<p>Bersacapavir (JNJ-56136379) is an in vitro modulator of hepatitis B virus capsid assembly that inhibits HBV replication.</p>

<p>ERCC1-XPF-IN-2: Nucleotide repair active, boosts cisplatin, inhibits ERCC1-XPF (IC50: 0.6 μM).</p>

<p>Galocitabine (Neofrutulon), a thymidylate synthase inhibitor, is used potentially for the treatment of cancer.</p>

<p>Talviraline (Bay 10-8979) is an RNA-induced DNA polymerase inhibitor.Talviraline is a potent inhibitor of HIV-1-induced cell killing and HIV-1 replication in a</p>

<p>NIOCH 14 is an orally available antiviral compound that inhibits exocorticoviruses, poxviruses, and smallpox viruses.</p>

Uprifosbuvir is an inhibitor of uridine nucleotide analog HCV NS5B polymerase.

N-(2-Hydroxypropyl)methacrylamide is used in the synthesis of copolymers for the targeted delivery of antileishmanial agents in Visceral leishmaniasis.

TTP-8307 is an antiviral compound that inhibits the replication of rhinoviruses and enteroviruses and is used in the study of viral infections.

<p>Isatin-β-thiosemicarbazone is a potent inhibitor of herpes simplex virus (HSV).</p>

<p>Antibacterial compound 2 is a potent antimicrobial agent effective against many human veterinary pathogens, inhibiting multi-drug resistant staphylococci,</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>Balapiravir HCl, an NS5B inhibitor, is used potentially for the treatment of HCV infection.</p>

<p>FWM-4 is a potent inhibitor of SARS-COV-2 NSP13 decapping enzyme.</p>

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

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

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

<p>L 680833 is an orally active monocyclic beta-lactam human polymorphonuclear leukocyte elastase inhibitor.</p>

<p>Antiparasitic agent-8 (Compound 9) exhibits potent antiparasitic activity against Hymenolepis nana, while demonstrating low levels of cytotoxicity [1].</p>

<p>AZD-7295 (A-689) is an NS5A inhibitor that may be used to treat HCV infection.</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>Murabutide, a safe synthetic immunomodulator, diminishes the expression of CD4 and CCR5 receptors and promotes the secretion of high levels of beta-chemokines,</p>

Urease Inhibitor 07 is an isosubstituted metalloproteinase inhibitor with potential activity against Mycobacterium tuberculosis strain H37Rv.

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

<p>Du011 is a biogenesis inhibitor of the E.</p>

<p>GSK3839919A is a potent allosteric inhibitor of HIV-1 integrase [1].</p>

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

<p>VT-1598 is a novel, selective, orally active fungal CYP51 inhibitor. VT-1598 exhibits antifungal effects against Candida albicans.</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>Myxopyronin A is an inhibitor of bacterial RNA polymerase.</p>

<p>Variculanol, a compound with antimicrobial, anticancer, and anti-HCV NS3/4A protease properties, is derived from the marine fungus Aspergillus versicolor [1].</p>

<p>Besifovir Dipivoxil maleate, an oral HBV prodrug (LB80380), suppresses HBV DNA in naive and lamivudine-resistant CHB cases.</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>RAD51-IN-4, a potent RAD51 inhibitor, may be useful in researching mitochondrial defect-related conditions.</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>Compound 5b, an antibacterial, effectively targets MRSA and disrupts bacterial membranes and PG synthesis.</p>

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

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

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

<p>Cladosporin, from Cladosporium cladosporioid fungus, halts dermatophyte growth on agar at 75 μg/mL.</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>Teropavimab (3BNC117-LS), an antibody, is utilized in the research of HIV infection [1].</p>

<p>PTC725 is a selective HCV 1b replicons inhibitor. It has been shown to target the nonstructural protein 4B.</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>AZ-27 is a respiratory syncytial virus inhibitor which differentially inhibits different polymerase activities at the promoter.</p>

<p>MC-VC-PAB-Cyclohexanediamine-Thailanstatin A is a spliceostatin analog and a drug-linker conjugate for antibody-drug conjugates (ADC), comprising the cytotoxic</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>HIV-1 inhibitor-3 is an HIV infection inhibitor.</p>

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

Icofungipen is an oral antifungals with active against Candida species.

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

<p>HBV-IN-6 is a potent inhibitor of HBV (EC50: 287.9 nM).</p>

<p>Talviraline (HBY 097) inhibits HIV-1 replication and reduces cell death in various cells and immune cells.</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>Yimitasvir diphosphate, also known as Emitasvir, is an orally-administered inhibitor of the hepatitis C virus (HCV) nonstructural protein 5A (NS5A).</p>

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

<p>Capravirine, a non-nucleoside reverse transcriptase inhibitor, is used potentially for the treatment of HIV infection.</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>Bio-AMS is a potent inhibitor of bacterial biotin protein ligase, exhibiting selective activity against Mycobacterium tuberculosis (Mtb) and disrupting fatty</p>

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

<p>Aranciamycin (Compound 1), an anthracycline antibiotic, exhibits collagenase inhibitory activity (IC50 3.7*10^-7 M) and can inhibit DNA synthesis in tumor cells</p>

<p>Quorum Sensing-IN-2 (compound 23e) is a quorum sensing inhibitor that curtails bacterial pathogenicity without impeding growth.</p>

<p>53BP1-binding protein 1 (53BP1) engages with dimethylated lysine 20 on histone 4 (H4K20me2) through its tandem tudor domains within a homodimer configuration, crucial for the DNA damage response. UNC2170, a micromolar 53BP1 ligand, selectively interacts with this site, demonstrating at least 17-fold preference for 53BP1 over similar proteins. This interaction occurs in a pocket formed by the 53BP1's tudor domains. Moreover, UNC2170 acts as an antagonist to 53BP1 in cellular lysates, effectively inhibiting class switch recombination, a process dependent on the functional 53BP1 tudor domain, thus confirming its cellular activity.</p>

<p>WQ 2743 is a potent agent of antimicrobial.</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>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>Antibacterial Agent 135 (example 7) effectively inhibits various bacteria, including P.</p>

HOE961, a diacetate ester prodrug of S2242, is an oral anti-orthopoxvirus agent effective against cowpox.

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

<p>1R-cis-Permethrin, an insecticide and neurotoxin, acts on neuron membranes by extending the activation of sodium channels [1].</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>12R-LOX-IN-1 (Compound 4a), with an IC50 of 28.25 µM, is an inhibitor of 12R-LOX.</p>

<p>EHNA hydrochloride is a PDE2 and ADA inhibitor with anticancer activity, increasing intracellular adenosine concentration in a treatment time-dependent manner.</p>

<p>SLU-10482, an antiparasitic agent, effectively reduces C.</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>Methyl 3,4-dimethoxycinnamate impedes uredospore germination and concurrently inhibits global DNA methylation in Hep3B cells [1] [2].</p>

<p>1,8-Dichloroanthraquinone, a derivative of anthraquinone, effectively inhibits sulfide production in sulfate-reducing bacteria [1].</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>Bavtavirine is a non-nucleoside reverse HIV-1 transcriptase inhibitor (NNRTIs),inhibits HIV replication by preventing the transcription of viral RNA into DNA.</p>

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

<p>GlcNAcstatin, a selective glucoimidazole-based inhibitor of bacterial O-GlcNAcase, exhibits a K_i value of 4.6 pM and demonstrates a specificity that is 100,000</p>

<p>Tuberculosis inhibitor 8 (compound 3b), a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative, exhibits potent activity against both Mycobacterium</p>

<p>Antituberculosis Agent-1 (Compound 8a) is an effective antituberculosis agent, demonstrating a minimum inhibitory concentration (MIC) of 3.84 μg/mL against</p>

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

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

Galidesivir hydrochloride is an inhibitor of viral RNA-dependent RNA polymerase (RdRp). It inhibits SARS-CoV-2 by tightly binding to its RdRp.

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