Ombuoside is a glycoside ombuoside isolated from Gynostemma pentaphyllum.Ombuoside has antimicrobial activity against several strains of gram-positive and gram-negative bacteria and the yeast Candida albicans[1]. Ombuoside has antioxidant effects by scavenging free radicals and ROS[2].
Vulpinic acid, a lichen metabolite, decreases H2O2-induced ROS production, oxidative stress and oxidative stress-related damages in human umbilical vein endothelial cells (HUVEC). Vulpinic acid is active against staphylococci, enterococci, and anaerobic bacteria.Vulpinic acid has the potential for atherosclerosis research[1][2].
14α-Demethylase/DNA Gyrase-IN-2 (Compound 6a) is a potent inhibitor of 14α-Demethylase/DNA Gyrase. 14α-Demethylase/DNA Gyrase-IN-2 has antimicrobial activities[1].
Ianthelliformisamine B diTFA is a bromotyrosine-derived antibacterial agent. Ianthelliformisamine B diTFA is against E. coli and S. aureus strains with MICs of 14.5 μM and 144.7 μM[1].
1-Deacetylnimbolinin B is a nimbolinin-type limonoid isolated from the fruits of Melia toosendan. Limonoids are a class of highly oxygenated nortriterpenoids that exhibit insecticidal, antifungal, nematicidal and cytotoxic properties[1].
Ozenoxacin is a nonfluorinated quinolone antibacterial, which shows potent activities against the main microorganisms isolated from skin and soft tissue infections.
DU011 is a noncanonical anti-infective agent and small-molecule inhibitor of capsule biogenesis, targets MprA (Kd=30 nM), a MarR family transcriptional repressor of multidrug efflux pumps, inhibits capsule expression in E. coli.DU011 does not alter Escherichia coli antibiotic resistance and has significantly enhanced inhibition of capsule expression, compared with other proposed MprA ligands, such as salicylate and 2,4-dinitrophenol (DNP).
Patchouli alcohol is a natural tricyclic sesquiterpene extracted from Pogostemon cablin (Blanco) Benth, and exhibits anti-Helicobacter pylori and anti-inflammatory properties[1].
Bleomycin sulfate is a DNA synthesis inhibitor with potent antitumor activity.
Cefmenoxime (SCE-1365) is a new semisynthetic cephalosporin antibiotic. Cefmenoxime has antibacterial activity against a wide variety of gram-positive and gram-negative bacteria[1][2].
Anti-MRSA agent 8 (Compound 7g) is a DAPG derivative with strong antibacterial activity. Anti-MRSA agent 8 assertes its activity by targeting bacterial cell membranes. Anti-MRSA agent 8 can be used for the research of methicillin-resistant Staphylococcus aureus (MRSA)[1].
Metallo-β-lactamase-IN-5 (compound 5c) is a potent metallo-β-lactamases (MBL) inhibitor. Metallo-β-lactamase-IN-5 shows inhibitory activity against MBLs NDM-1 and VIM-1. Metallo-β-lactamase-IN-5 inhibits HUVECs with an IC50 of 45 μg/mL. Metallo-β-lactamase-IN-5 plus Imipenem exhibits synergistic antimicrobial activity[1].
4-Hydroxybenzoic acid, a phenolic derivative of benzoic acid, could inhibit most gram-positive and some gram-negative bacteria, with an IC50 of 160 μg/mL.
Antibacterial agent 99 (compound 7b) is a potent antibacterial agent. Antibacterial agent 99 shows significant antibacterial and antifungal activity. Antibacterial agent 99 dose not show haemolytic activity[1].
Nucleocidin is an antitrypanosomal antibiotic, inhibiting the transfer of labeled amino acid from S-RNA to protein.
Monogalactosyl diglyceride is a antimicrobial. Monogalactosyl diglyceride has antibacterial activity and antifungal activity in vitro[1].
HCV-IN-3 is a hepatitis C virus (HCV) NS3/4a protein inhibitor, with an IC50 of 20 μM, a Kd of 29 μM.
Anserinone B is an antifungal and antibacterial benzoquinone. Anserinone B causes radial growth reductions of 50% and 37% against S.fimicola and A. furfuraceus, respectively. Anserinones B also displays moderate cytotoxicity in the NCI’s 60 human tumor cell line panel (GI50=4.4 µg/mL)[1].
Tenofovir diphosphate triethylamine (TFV-DP triethylamine) is a competitive DNA polymerases inhibitor (with respect to dATP) and a substrate of HIV type 1 (HIV-1) reverse transcriptase (RT)[1].
Ceftobiprole medocaril is the parenteral prodrug of Ceftobiprole (HY-112579). Ceftobiprole is a broad-spectrum cephalosporin with activity against Methicillin-resistant staphylococcus aureus (MRSA).
BC-11 hydrobromide is a selective TMPRSS2 inhibitor (TMPRSS2 is a key host cellular factor for viral entry and SARS-CoV-2 pathogenesis), and a selective urokinase (uPA) inhibitor (IC50=8.2 μM). BC-11 hydrobromide is cytotoxic to triple-negative MDA-MB231 breast cancer cells. BC-11 hydrobromide is used in research on viral infections and cancer[1][2][3].
Hygromycin A is a Borrelia burgdorferi-selective antibiotic. Hygromycin A is a spirochete-specific antibacterial that is conducive to gut health. Hygromycin A can be used for Lyme disease research[1].
Fumagillin(NSC9168) is a complex biomolecule and used as an antimicrobial agent.Target: AntiparasiticFumagillin is an active amebicide and anti-infective isolated from the fungus Aspergillus fumigatus. Fumagillin does exhibit some side effects that have deterred its acceptance as a viable treatment, but the current body of research on the synthesis of novel analogs of this molecule shows an exciting and promising revival of this drug as both an anti-infective and antiangiogenic agent [1].
Trimetrexate(CI-898) is a potent competitive inhibitor of bacterial, protozoan, and mammalian dihydrofolate reductase.IC50 value:Target: Antibiotic Trimetrexate therapy had minimal toxicity; transient neutropenia or thrombocytopenia occurred in 12 patients and mild elevation of serum aminotransferases in 4. We conclude that the combination of trimetrexate and leucovorin is safe and effective for the initial treatment of pneumocystis pneumonia in patients with AIDS and for the treatment of patients with intolerance or lack of response to standard therapies [1]. In noncomparative trials trimetrexate was effective in the treatment of P. carinii pneumonia (PCP) in patients with AIDS who were intolerant of or refractory to cotrimoxazole (trimethoprim/sulfamethoxazole) and pentamidine treatment. In these patients, 2- to 4-week survival rates of 48 to 69% were reported. In a comparative trial in the initial therapy of PCP, trimetrexate was less effective than cotrimoxazole in moderate to severe disease as evidenced by a significantly higher failure rate [2]. trimetrexate plus leucovorin was effective, albeit inferior to TMP-SMZ, for moderately severe P. carinii pneumonia but was better tolerated than TMP-SMZ [3].
Cap-dependent endonuclease-IN-25 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-25 is a macrocyclic pyridotriazine derivative. Cap-dependent endonuclease-IN-25 has the potential for the research of viral infections caused by viruses belonging to the Orthomyxoviridae family (extracted from patent WO2020075080A1, compound 4)[1].
Flagelin 22, a fragment of bacterial flagellin, is an effective elicitor in both plants and algae.
Antifungal agent 51 (5c) has potent antifungal activity, especially against Candida albicans FDC 151 , Candida parapsilosis ATCC 22019 and Candida tropicalis FDC 138, with the MIC value is less than 0.063 μg/mL, and it has low toxicity to cells and no carcinogenicity[1].
Antimycobacterial agent-2 (compound 58) is a potent antimycobacterial agent. Antimycobacterial agent-2 shows anti-mycobacterial activities with an MIC99 of 0.8 µM for Mycobacterium tuberculosis (M.tb) H37Rv. Antimycobacterial agent-2 shows cytotoxic activities with an IC50 of48.1 µM for CHO cells[1].
Rufloxacin hydrochloride (MF-934 hydrochloride) is a fluoroquinolone antibacterial, inhibits B-cell differentiation in human mononuclear cells, inhibits Topo.
Cefpiramide (SM-1652) free acid is a semisynthetic cephalosporin with broad-spectrum antibacterial activity. Cefpiramide free acid shows strong antibacterial effect on both gram-positive bacteria and gram-negative bacteria. Cefpiramide free acid is moderately susceptible to β-lactamase[1][2].