Microbiologia/Virologia

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

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

<p>WRN Inhibitor 1 (example 7) is an inhibitor of the Werner Syndrome ATP-dependent helicase enzyme (WRN), selectively targeting its helicase domain.</p>

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

<p>(-)-Verazine is an antifungal agent isolated from the dried roots and rhizome of Veratrum maackii Regel, which induces DNA damage in the cerebellum and cerebral</p>

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

<p>L-696229: specific HIV-1 RT inhibitor, blocks viral spread in various cells.</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>Compound 158 (6c), a Micrococcin analogue, serves as an antibacterial agent effective against impetigo and Clostridium difficile infection (CDI) [1].</p>

<p>CPFX2090, a cephalosporin antibacterial compound.</p>

<p>SARS-CoV-2-IN-66 (1), a derivative of vitamin K, functions as an inhibitor of SARS-CoV-2, exhibiting an effective concentration (EC50) of 70.8 μM in VeroE6/</p>

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

<p>BILR-355 is a reverse transcriptase inhibitor.</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>Valtorcitabine dihydrochloride, a DNA polymerase inhibitor, is used potentially for the treatment of HBV infection.</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>SA09-Cu is a potent, noncompetitive inhibitor of NDM-1, with an IC50 of 9.6 nM.</p>

<p>Cap-dependent endonuclease-IN-13 is a potent inhibitor of cap-dependent endonuclease (CEN) and shows research potential against influenza virus infection (</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>ISPA-28: reversible PSAC antagonist via direct CLAG3 binding.</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>HBV-IN-12 is a potent inhibitor of hepatitis B surface antigen (HBsAg).</p>

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

<p>BMY-43748 is an antibacterial compound with great in vitro and in vivo antibacterial activity.</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>Palinavir is an antiviral, it inhibits HIV-1 protease.</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>Pradimicin A derivative 26 exhibits antifungal, antiviral, and antiparasitic properties by attaching to d-mannose (Man)-rich glycans in pathogenic organisms [1</p>

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

<p>NEU-730, a novel inhibitor of TbrPDEB1, shows modest inhibition of T. brucei proliferation.</p>

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

<p>Antibacterial 91: Inhibits aaRS, IC50 2.10μM vs. S. enterica ThrRS, has antibacterial properties. [1]</p>

<p>OfChi-h-IN-2 (compound TQ19) is a potent inhibitor of OfChi-h, exhibiting a K i of 0.33 μM, and significantly impairs the growth and development of Ostrinia</p>

<p>R 87366 is used as a water-soluble HIV protease inhibitor.</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>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>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>Variculanol, a compound with antimicrobial, anticancer, and anti-HCV NS3/4A protease properties, is derived from the marine fungus Aspergillus versicolor [1].</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>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>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>DQn-1, a potent antifolate, demonstrates efficacy against Mycobacterium tuberculosis (Mtb) with an MIC 90 of 0.03 µM.</p>

<p>Debrisoquin (Isocaramidine) is a TMPRSS2 inhibitor that prevents SARS-CoV-2 from entering human lung cells through TMPRSS2-dependent pathways, exhibiting an</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>Oxamniquine is an effective compound for the treatment of schistosomiasis.</p>

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

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

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

<p>SARS-CoV-2-IN-62 (Compound R3b) effectively inhibits SARS-CoV-2 replication in Vero E6 and Calu-3 cells, demonstrating low cytotoxicity and EC50 values of 2.97</p>

<p>β-Lactamase-IN-2 is an inhibitor of β-Lactamase with anti-microbial and anti-bacterial effects.</p>

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

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

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

<p>A 33853 is an antibiotic isolated from culture broth of Streptomyces sp.</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>COH1 is a ribonucleotide reductase (RR) inhibitor utilized in research pertaining to cancer, mitochondrial diseases, and neurodegenerative disorders [1].</p>

<p>Sulfisoxazole acetyl (Gantrisin) is an agent with antibacterial activity.</p>

<p>Antibacterial compound 2 is a potent antimicrobial agent effective against many human veterinary pathogens, inhibiting multi-drug resistant staphylococci,</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>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>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>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>FR194738 free base inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC50 of 9.8 nM. </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>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>Compound 5b, an antibacterial, effectively targets MRSA and disrupts bacterial membranes and PG synthesis.</p>

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

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

<p>Cyclic HPMPC: Potent antiviral, raises O2 in mice with lethal vaccinia, lowers guinea pig CMV replication.</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>UNC-2170 (UNC2170 Maleate) is the methyl-lysine binding protein, 53BP1 ligand.</p>

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

<p>AZ-27 is a respiratory syncytial virus inhibitor which differentially inhibits different polymerase activities at the promoter.</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>MF 5137 is an effective antimicrobial agent.</p>

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

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

<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>Brevicompanine B: fungal metabolite, regulates plant growth/circadian rhythm, inhibits Arabidopsis roots, affects gene transcription, anti-P. falciparum.</p>

Antitrypanosomal agent 14 (Compound 1), a potent T.

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

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

<p>T145 halts key bacteria growth at sub μg/ml, deters resistance, and may enhance drug lifespan.</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>LY 173013 is a bicyclic pyrazolidinone, it has antibacterial properties.</p>

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

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

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

<p>Tobevibart, an IgG1-lambda humanized monoclonal antibody targeting the hepatitis B virus (HBV) surface envelope protein, exhibits antiviral activity [1].</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>Pexiganan acetate (MSI 78), a 22-residue peptide analogue of magainin 2, disrupts bacterial membranes or walls, leading to antibacterial activity.</p>

<p>HIV-1 inhibitor-10 is a nanomolar HIV-1 maturation inhibitor.</p>

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

<p>Talviraline (HBY 097) inhibits HIV-1 replication and reduces cell death in various cells and immune cells.</p>

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

<p>Alteconazole is an antifungal drug.</p>

<p>Indinavir, threo- is a protease inhibitor utilized as a component of highly active antiretroviral treatment to HIV/AIDS.</p>

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

<p>Berlopentin is splenopentin analog used to treat HIV-positive patients. It also has immunostimulatory properties.</p>