Drosocin is a biological active peptide. (Drosocin is a 19-mer cationic antimicrobial peptide from Drosophila melanogaster. In Drosophila native drosocin carries a disaccharide moiety attached to a threonine residue in mid-chain position. This synthetic drosocin peptide of identical amino acid sequence without the disaccharide has an activity several times lower than the native compound.)
Dexamethasone-4,6α,21,21-d4 is the deuterium labeled Dexamethasone-4,6α,21,21. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
QPX7728 bis-acetoxy methyl ester is a boronic acid β-lactamase inhibitor, exacted from WO2018005662A1, compound 42[1].
Antibacterial agent 130 is a 1,1-diarylthiogalactoside, used for targeting the Pseudomonas aeruginosa LecA. Antibacterial agent 130 shows high affinity toward LecA (Kd=1 μM). Antibacterial agent 130 has antibiofilm activity, but lacks bactericidal activity. LecA, a lectin and virulence factor from Pseudomonas aeruginosa involved in bacterial adhesion and biofilm formation[1].
BAL-30072, a siderophore sulfactam, is a monocyclic beta-lactam antibiotic, with activity against multiresistant gram-negative bacilli. BAL30072 shows MIC90 values of 4 μg/mL for MDR Acinetobacter spp. and 8 μg/mL for MDR P. aeruginosa, respectively[1][2].
Probenecid-d14 is the deuterium labeled Probenecid. Probenecid is a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Probenecid also inhibits pannexin 1 channels[1][2].
Raxibacumab (ABthrax) is a human IgG1 monoclonal antibody against Bacillus anthracis protective antigen (PA). Raxibacumab blocks the toxin’s deleterious effects by preventing binding of the protective antigen component of the anthrax toxin to its receptors in host cells, thereby blocking the toxin’s deleterious effects. Raxibacumab can be used for anti-anthrax research[1][2].
MRV03-070 is an inhibitor of colibactin-activating peptidase ClbP with an IC50 value of 69 nM, acts like biosynthetic precursor precolibactin[1].
Propineb (Zinc propylenebis) is a compound widely used in fruit and vegetables cultures, due to its large spectrum of activity against fungal plant diseases[1].
Mupirocin calcium hydrate is an orally active antibiotic isolated from Pseudomonas fluorescens. Mupirocin calcium hydrate apparently exerts its antimicrobial activity by reversibly inhibiting isoleucyl-transfer RNA, thereby inhibiting bacterial protein and RNA synthesis[1][2].
DHFR-IN-10 (compound 4c) is a potent DHFR inhibitor, with an IC50 of 4.21 μM for M. tuberculosis DHFR enzyme. DHFR-IN-10 exhibits potent antituberculosis efficiency[1].
Nimbin is a intermediate limonoid isolated from Azadirachta. Nimbin prevents tau aggregation and increases cell viability. Nimbin is effective inhibits the envelope protein of dengue virus. Nimbin has anti-inflammatory, antipyretic, antifungal, antihistamine, antiseptic, antioxidant, anti-cancer and anti-viral properties. Nimbin can across blood-brain barrier[1][2][3].
Neamine tetrahydrochloride, a degradation product of Neomycin, is a broad-spectrum aminoglycoside antibiotic. Neamine tetrahydrochloride is an anti-angiogenesis agent targeting angiogenin. Neamine tetrahydrochloride has potent antibacterial, antitumor and neuroprotective activities[1][2].
Norchelerythrine is an alkaloid isolated from the roots of Zanthoxylum capense with antibacterial activity against gram-positive and gram-negative bacteria. Norchelerythrine exhibits inhibitory activity against Staphylococcus aureus, Pseudomonas aeruginosa, and Enterococcus faecalis and Escherichia coli with MIC values >50 µg/mL[1].
Oleuropeic acid 8-O-glucoside is a terpenic compound, that can be isolated from twigs with leaves of Juniperus communis var. depressa. Oleuropeic acid 8-O-glucoside shows antibacterial activity against three strains of Helicobacter pylori (NCTC11637, NCTC11916, and OCO1), with MIC of 100 μg/mL all[1].
Decamethoxine (Septefril) is a cationic gemini surfactant. Decamethoxine exhibits strong bactericidal and fungicidal effects. Decamethoxine modifies the permeability of the microbial cell membrane, resulting in the destruction and death of diverse microorganisms[1][2].
Neomycin sulfate is an aminoglycoside antibiotic used for preventing or treating bacterial infections.
Narasin sodium is a cationic ionophore and coccidiostat agent. Narasin inhibits NF-κB signaling and induces tumor cells apoptosis. Narasin sodium has antimicrobial and anticancer activity[1].
Octenidine is a potent antibacterial agent, possessing activity against multidrug-resistant Gram-negative pathogens. Octenidine can inhibit the expression of biofilm genes and destroy the formation of biofilms[1][3].
Methylisothiazolinone hydrochloride is the constituent of the biocide Kathon CG. Methylisothiazolinone hydrochloride is an isothiazolone derivative widely used as a preservative. Methylisothiazolinone hydrochloride is also a moderate sensitizer and reacts with GSH[1][2].
Dehydroglaucine is a potent antimicrobial alkaloid[1].
Antimicrobial Compound 1 is an alkylpyridinium compound, with antimicrobial activity.
NSC309401 is an inhibitor of E. coli DHFR (IC50: 189 nM, KD: 14.57 nM)[1].
c[Arg-Arg-Arg-Arg-Dip-Dip-Dip] (Compound 8C) shows broad-spectrum activity against drug-resistant Gram-positive and Gram-negative bacteria, with MICs of 3.1, 3,1, 12.5, and 12.5 μg/mL for MRSA (ATCC BAA-1556), S. aureus (ATCC 29213), P. aeruginosa (ATCC 27883), and E. coli (ATCC 25922), respectively[1].
MRV03-037 is a selective colibactin-activated peptidase (ClbP) inhibitor that blocks the genotoxic effect of Colibactin (HY-145930) on eukaryotic cells. MRV03-037 prevents gut bacterial genotoxin production[1].
ML267 a potent Sfp phosphopantetheinyl transferase (PPTases) inhibitor with an IC50 of 0.29 μM. ML267 also inhibits AcpS-PPTase with an IC50 of 8.1 μM. ML267 possesses specific Gram-positive-targeted bactericidal activities[1].
TBA-354 is a potent anti-tuberculosis compound; maintains activity against Mycobacterium tuberculosis H37Rv isogenic monoresistant strains and clinical drug-sensitive and drug-resistant isolates.IC50 value:Target: Anti-tuberculosis agentin vitro: TBA-354 is narrow spectrum and bactericidal in vitro against replicating and nonreplicating Mycobacterium tuberculosis, with potency similar to that of delamanid and greater than that of PA-824. TBA-354 maintains activity against Mycobacterium tuberculosis H37Rv isogenic monoresistant strains and clinical drug-sensitive and drug-resistant isolates [1]. TBA-354 is 5 to 10 times more potent than PA-824, but selected mutants are cross-resistant to PA-824 and delamanid. TBA-354 is 2 to 4 times more potent than PA-824 when combined with bedaquiline, and when administered at a dose equivalent to that of PA-824, TBA-354 demonstrated superior sterilizing efficacy [2].in vivo: TBA-354 has high bioavailability and a long elimination half-life. In vitro studies suggest a low risk of drug-drug interactions. Low-dose aerosol infection models of acute and chronic murine tuberculosis reveal time- and dose-dependent in vivo bactericidal activity that is at least as potent as that of delamanid and more potent than that of PA-824.
Hygromycin B is an aminoglycoside antibiotic active against prokaryotic and eukaryotic cells.
4aα,7α,7aα-Nepetalactone exhibits antibacterial activity, and inhibits Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Salmonella typhi and Enterococcus faecalis.
α-Terpineol is isolated from Eucalyptus globulus Labill, exhibits strong antimicrobial activity against periodontopathic and cariogenic bacteria[1].α-Terpineol possesses antifungal activity against T. mentagrophytes, and the activity might lead to irreversible cellular disruption[2].