Microbiologia/Virologia

<p>Paclobutrazol ((R,R)-paclobutrazol) is a triazole-containing plant growth retardant that is known to inhibit the biosynthesis of gibberellins.1,2It also has</p>

<p>Destruxin A is a cyclic hexadepsipeptide produced by fungus causing paralysis and death in insects.</p>

<p>WAY-324208 shows antifungal properties against S. dermatitidis (skin-infecting fungi), with activity against other fungi to be explored.</p>

<p>SARS-CoV-2 nsp13-IN-7 (Compound 6r) is an inhibitor of SARS-CoV-2 nsp13, with an IC50 of 0.28 μM. This compound disrupts the helicase function of nsp13 by binding to its 5' RNA site and ATP binding site, and it serves as a lead compound for developing antiviral drugs targeting SARS-CoV-2 nsp13.</p>

<p>Ecubectedin (PM14), a derivative of ecteinascidins family, has antitumor and antimicrobial properties.</p>

<p>Mycobactin P is one of iron(III) chelating compounds produced by most species of Mycobacteria which act as growth factors.</p>

<p>HIV protease-IN-1 (compound 1·succinate), a potent non-peptidic inhibitor of HIV protease, is utilized for AIDS research [1].</p>

<p>Dehydrolycopene, a major SGA in tomatoes' green fruits, leaves, and flowers, targets bacteria, fungi, insects, and animals.</p>

<p>Clofarabine-5'-diphosphate (Clofarabine-DP) is a metabolite resulting from the phosphorylation of Clofarabine by deoxycytidine kinase (dCK). It can undergo further phosphorylation to become Clofarabine-5'-triphosphate, exhibiting cytotoxicity in cancer cells by inhibiting DNA synthesis and repair.</p>

<p>SARS-CoV-2-IN-25 disodium, a potent inhibitor, blocks SARS-CoV-2 spike interaction with IC50 of 1.6 μM.</p>

<p>Compound 16 is an antimicrobial with 4-8 μg/mL MIC, effective on gram-positive/negative bacteria and has anti-inflammatory properties.</p>

<p>SARS-CoV-2-IN-46 is a SARS-CoV-2 inhibitor.</p>

<p>Methyl quinoline-2-carboxylate (Methyl 2-quinolinecarboxylate) inhibits the binding of Mycobacterium tuberculosis.</p>

<p>Gemifloxacin is a fluoronaphthyridone with strong antibacterial effect.</p>

<p>FtsZ-IN-5: Potent inhibitor blocking bacterial division, low resistance and toxicity, enhances FtsZ polymerization.</p>

<p>SDH-IN-2: Strong SDH blocker (IC50 0.55 μg/mL), antifungal; EC50 3.82-9.81 μg/mL against plant fungi.</p>

<p>4-(2-Aminoethyl)amino-7-chloroquinoline (N1-(7-Chloroquinolin-4-yl)ethane-1,2-diamine) has potential anthelmintic and antitumor activity for the study of</p>

<p>Spike protein mRNA for COVID-19 enables protein expression, assesses RNA delivery, translation, cell health, and is key for virus entry and vaccine targets.</p>

<p>Cefazaflur is a novel semi-synthetic cephalosporin derivative that can be used as an Antibiotic agent.</p>

<p>Antifungal Antibacterial agent 84 targets CNB1 to thwart C. albicans biofilm.</p>

<p>Ascochin, an isocoumarin derivative and fungal metabolite identified in Ascochyta, demonstrates antimicrobial activity. At a concentration of 0.5 mg/disc, it inhibits Bacillus megaterium (the bacterium), Mycosphaerella violaceum (the plant pathogenic fungus), and Chlorella fusca (the alga) in agar diffusion assays.</p>

<p>Antibacterial agent 12 targets antibiotic-susceptible/resistant Gram-positive bacteria.</p>

<p>5’-O-DMT-2’-O-TBDMS-Ac-rC is a modified nucleoside and can be used to synthesize DNA or RNA.</p>

<p>HBV core protein found in nucleus and cytoplasm of infected hepatocytes; phosphorylation regulates nuclear presence by cell cycle.</p>

<p>Nv-CATH, an antibacterial peptide derived from frogs, exhibits broad-spectrum activity against both gram-positive and gram-negative bacteria, and significantly</p>

<p>Amphotericin B trihydrate, a polyene antibiotic, is derived from Streptomyces nodosus fermenter cultures. It exhibits antileishmanial properties.</p>

<p>Quinaldopeptin: a quinomycin antibiotic, combats various bacteria, cytotoxic to cells, aids in P388 leukemia mouse survival, intercalates DNA.</p>

<p>Picarbutrazox: potent pesticide/fungicide for corn/soybean against Pythium/Phytophthora.</p>

<p>Gamma-Glutamyl Transferase-IN-2 (compound 4dq), a β-carboline 1-hydrazide inhibitor, exhibits both antifungal and antibacterial properties by targeting</p>

<p>Biotin-PEG3-Mal (Biotin-PEG3-NH-Mal) is a biotin-labeled PROTAC linker belonging to the PEG class that can be used to synthesize PROTAC molecules.</p>

<p>A 16316-C is a water soluble basic antibiotic, it is isolated from Streptoverticillium eurocidicus.</p>

<p>HIV-1 inhibitor-11, a fused pyridine ring derivative, is a HIV-1 inhibitor.</p>

<p>EFdA-TP: potent HIV-1 RT inhibitor; acts via immediate/delayed chain termination (ICT/DCT) and multiple pathways.</p>

<p>Omadacycline: an aminomethylcycline antibiotic, cidal against four Streptococcus pneumoniae strains.</p>

<p>SARS-CoV-2 Mpro-IN-36 (Compound 6d) is an inhibitor of SARS-CoV-2 Mpro with an IC50 of 110 nM. This compound demonstrates antiviral activity with an EC50 of 1.6 μM.</p>

<p>XT-4, an antimicrobial peptide originating from the skin secretions of Xenopus tropicalis, exhibits potent activity against E.</p>

<p>Eprinomectin B1b is a minor component and belongs to the avermectin family of insecticides and anthelmintics.</p>

<p>Maximin 1, an antimicrobial peptide originating from the skin secretions of Bombina maxima, exhibits cytotoxicity against tumor cells and possesses spermicidal</p>

<p>PT-129 is a RPOTAC degrader that targets the G3BP1/2NTF2 domain (protein-RNA interaction site), facilitating the breakdown of intracellular stress granules. It prevents the formation of stress granules in stressed cells and deconstructs existing ones, thereby disrupting ATF4 transmission and inhibiting cancer cell proliferation. Stress granules (SGs) are membraneless cytoplasmic compartments formed under stress, which aid in the transfer of ATF4 from fibroblasts to tumor cells, promoting fibroblast-related tumor growth. G3BP1/2 serve as central proteins in the SG network, and inhibiting them may reduce the stress resilience of cancer cells within the tumor microenvironment. PT-129 consists of a target protein ligand (red part) G3BP1/2-Targeting ligand-1, an E3 ligase ligand (blue part) Thalidomide 4-fluoride, and a PROTAC linker (black part) Amino-PEG3-C2-acid; the E3 ligase ligand and linker form the complex Thalidomide-NH-PEG3-propionic acid.</p>

<p>CHEMBL1380345 fights S. aureus, B. cereus, E. coli; pMICs: 3.64, 3.56, 3.70.</p>

<p>Flagelin 22, a bacterial flagellin fragment, serves as a potent elicitor for plants and algae.</p>

<p>Thanatin acetate is a cationic peptide with antimicrobial activity, inhibiting bacterial and fungal growth.</p>

<p>Dodecamethylpentasiloxane can be used as a bed bug insecticide. Dodecamethylpentasiloxane is a component of siloxane and can be used as silicone oil.</p>

<p>Lankacidinol A is a metabolite of macrolide antibiotic.</p>

<p>Oligomycin E, a Streptomyces metabolite, has weak antifungal properties but strong Gram-positive and HeLa cell antitumor effects (IC50=14 ng/ml).</p>

<p>Pristinamycin, from Streptomyces pristinaespiralis, is a streptogramin antibiotic targeting Gram-positive and resistant bacteria like MRSA.</p>

<p>Antiviralagent 66 (Compound 60) serves as an inhibitor of filoviruses (Filovirus), effectively suppressing pseudoviruses of Ebola, Marburg, Zaire, Sudan, Bundibugyo, Reston, and Tai Forest, with EC50 values of 0.16, 2.24, 0.16, 0.89, 0.21, 0.21, and 0.11 μM, respectively.</p>

<p>Diclobutrazol: potent systemic fungicide against rusts, mildews, and crop diseases.</p>

<p>Isatropolone A from Streptomyces Gö66 has a 1,5-diketone; it's potent against Leishmania with IC50 of 0.5μM.</p>

<p>Ochratoxin C is a toxic metabolite from Aspergillus orchraceus.</p>