Microbiologia/Virologia

<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>RSV L-protein-IN-2 (Compound A), a noncompetitive inhibitor of the RSV polymerase (IC50: 4.5 μM), exhibits antiviral activity against long RSV strains (EC50: 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>FWM-4 is a potent inhibitor of SARS-COV-2 NSP13 decapping enzyme.</p>

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

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

<p>Antituberculosis agent-6: potent against M. tuberculosis (MIC 3.49 μM), antifungal (MIC 62.5 μM), high GI absorption.</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>Ganfeborole HCl (GSK3036656 HCl) is a compound with anti-tuberculosis activity and is an inhibitor of Mycobacterium tuberculosis (Mtb) leucyl-tRNA synthetase.</p>

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

<p>DU-34569 Maleate, an antiviral agent, acts against influenza A, parainfluenza Sendai, coxsackie A21, and rhinovirus.</p>

<p>HBV-IN-30, a flavone derivative, inhibits cccDNA in HBV research.</p>

<p>AU1235 is a Mycobacterium tuberculosis inhibitor.</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>5,11-methenyltetrahydrohomofolate blocks GAR &amp; AIR transformylase; used as an anti-purine drug.</p>

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

<p>Prochloraz manganese, an antifungal agent utilized in the agricultural sectors [1], serves to protect crops by inhibiting fungal growth.</p>

<p>L-697661, a reverse transcriptase inhibitor, is used potentially for the treatment of HIV infection.</p>

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

<p>Zndm19 is an inhibitor of New Delhi Metallo-β-lactamase-1 (NDM-1), utilized in researching drug-resistant bacterial infections [1].</p>

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

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

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

<p>Propamidine acts as a covalent inhibitor of TMPRSS2 and exhibits antibacterial properties. [1]</p>

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

<p>ZINC03129319 is an inhibitor of dengue virus (DENV) NS2B-NS3 protease.</p>

<p>Pyrethrin II, an active insecticidal component of pyrethrins, is a biogenic insecticide derived from Chrysanthemum cinerariifolium [1].</p>

<p>NSC 288387, a pan-flavivirus MTase inhibitor, binds to the SAM-binding pocket and effectively inhibits Zika virus (ZIKV) with an IC50 of 0.2 μM, also preventing</p>

<p>Antibacterial agent 92 inhibits Salmonella's aaRS; IC50 of 0.58 μM for Se ThrRS. Exhibits antibacterial effects.</p>

<p>DB-766: Chagas' treatment candidate with potent, selective trypanocidal action. IC50: 60 nM (bloodstream), 25 nM (intracellular). Promising new lead.</p>

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

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

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

<p>Laninamivir Octanoate Monohydrate is a neuraminidase inhibitor.</p>

Inz-5 is a fungal-selective inhibitor of mitochondrial cytochrome bc1. Inz-5 impairs fungal virulence. It also prevents the evolution of drug resistance.

<p>Pexiganan acetate (MSI 78), a 22-residue peptide analogue of magainin 2, disrupts bacterial membranes or walls, leading to antibacterial activity.</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>Compound 6d (Antibacterial agent 159) is an antibiotic effective against impetigo and Clostridium difficile infection (CDI), with no observed recurrence for CDI</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>FAICAR (5-Formamidoimidazole-4-carboxamide ribotide), a purine nucleotide, plays a crucial role in metabolic processes.</p>

<p>XZ426 is a potent integrase strand transfer inhibitor with anti- HIV activity .</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>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>

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

<p>NVS-SM2 boosts SMN2 splicing, enhances exon 7 inclusion, and raises SMN protein levels orally.</p>

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

<p>(+)-Thienamycin, a powerful broad-spectrum antibacterial and β-lactamase inhibitor, is isolated from Streptomyces cattleya [1].</p>

Gusperimus trihydrochloride is a derivative of the antitumor antibiotic spergualin with immunosuppressant activity.

<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>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>COH1 is a ribonucleotide reductase (RR) inhibitor utilized in research pertaining to cancer, mitochondrial diseases, and neurodegenerative disorders [1].</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>3-Cyanovinylcarbazole phosphoramidite: an antiviral, hinders viral DNA synthesis, modifies ribonucleotides.</p>

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

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

<p>NIK-250 is a P-glycoprotein inhibitor. NIK250 could reverse multidrug resistance in human glioma cells.</p>

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

<p>PYR01 is a potent nonnucleoside reverse transcriptase inhibitor of HIV-1 and concurrently acts as a targeted activator to eliminate cells expressing HIV-1 [1].</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>HEC72702: New HBV capsid inhibitor, from GLS4. No CYP1A2, CYP3A4, CYP2B6 induction at 10μM.</p>

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

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

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

<p>L 694746 is an inhibitor of HIV-1 protease.</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>Votoplam functions as a gene splicing modulator, employed in the inhibition of Huntington's disease [1].</p>

<p>JNJ4796 is an oral fusion inhibitor that neutralizes influenza A group 1 by blocking HA-mediated fusion, mimicking bnAbs.</p>

<p>Linvencorvir is a hepatitis B virus (HBV) core protein variant modifier used to treat chronic HBV infection.</p>

<p>SMN-C3 (MV8T2MCK57) is an orally active modulator of SMN2 splicing, and has the potential to treat spinal muscular atrophy (SMA).</p>

<p>MMV688533 has antimalarial activity.</p>

<p>Filibuvir (PF-00868554) inhibits HCV polymerase genotypes 1a/1b, EC50s 59 nM.</p>

<p>TCMDC-135051: Selective PfCLK3 inhibitor, low toxicity, halts parasite growth &amp; transmission; EC50=320 nM.</p>

<p>GSK3186899 is an inhibitor of Cdc2-related kinase 12 with an EC50 of 1.4 μM for L. donovani.</p>

<p>CWHM-1552 is an effective Plasmodium falciparum inhibitor. For the 3D7 and Dd2 strains, the IC50s are 51 nM and 53 nM.</p>

<p>Nesbuvir: HCV NS5B polymerase inhibitor, IC50 9 nM against HCV 1b replicon in liver cancer cells.</p>

<p>2,4′-Dichloroacetanilide (2-chloro-N-(4-chlorophenyl)acetamide) has antifungal activity and inhibits T. asteroides with a MIC value of 6.25 μg/mL.</p>

<p>Tenofovir amibufenamide (HS-10234) 是一种 Tenofovir 前药，是一种具有口服活性的抗病毒化合物。Tenofovir amibufenamide 对乙型肝炎病毒 (HBV)具有抑制作用，可用于慢性乙型肝炎 (CHB) 研究。</p>

<p>Thymectacin (NB 1011) is a selective thymidine synthase (TS) inhibitor with anticancer activity for the study of colon cancer and solid tumors.</p>

<p>Salicyl-AMS is an inhibitor of mycobacterium auxin biosynthesis that inhibits the growth of mycobacterium in the presence of iron deficiency in vitro.</p>

Contezolid (MRX-I) is an antibiotic with bactericidal activity and can be used to study tuberculosis.

<p>A7132 is an antibacterial agent and possesses broad and potent antibacterial activity.</p>

<p>ZY-19489: Antimalarial, potential single-dose cure, FDA orphan drug status.</p>

<p>S-Allylmercapturic Acid (N-Acetyl-S-allyl-L-cysteine) is a metabolite of S-allyl-L-cysteine present in black garlic, with potential anti-gout effects.</p>

<p>DHX9-IN-2 is an inhibitor targeting ATP-dependent RNA de-helicase A (DHX9) with anticancer and antitumor activity for cancer research.</p>

<p>Dehydroemetine, a synthetic emetine, treats amoebic infections and leishmaniasis, and resists metronidazole amoebiosis.</p>

<p>LNA-Adenosine (LNA-A) is a nucleoside analogue that acts as a ligand for adenosine A3 receptors.</p>

<p>Dermatan sulphate sodium (Chondroitin sulfate B sodium salt) is a linear sulfated polysaccharide, a glycosaminoglycan component of important proteoglycans.</p>

Ziresovir (RO-0529) is a respiratory syncytial virus fusion protein (RSV F) inhibitor that inhibits RSV and can be used to study syncytial virus sense.

CeMMEC1 is an inhibitor of BRD4, and also has a great affinity for TAF1(IC50=0.9 μM).

<p>Lomibuvir (VCH-222, VX-222) is an allosteric inhibitor of HCV NS5B with Kd 17 nM, blocks RNA elongation, EC50 5.2 nM for 1b/Con1.</p>