Moxifloxacin (Hydrochloride) is a synthetic fluoroquinolone antibiotic agent.Target: AntibacterialMoxifloxacin is an extended-spectrum fluoroquinolone which has improved coverage against gram-positive cocci and atypical pathogens compared with older fluoroquinolone agents, while retaining good activity against gram-negative bacteria. The antibacterial spectrum of moxifloxacin includes all major upper and lower respiratory tract pathogens; it is one of the most active fluoroquinolones against pneumococci, including penicillin- and macrolide-resistant strains [1]. Moxifloxacin has limited phototoxic potential. In clinical trials, moxifloxacin had clinical success rates of 88-97% and bacteriologic eradication rates of 90-97%. Moxifloxacin is a safe and effective antimicrobial that will be useful for treating acute sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia [2]. Moxifloxacin possibly stimulates lipid peroxidation and enhances phagocytosis, as depicted by MDA production and survival prolongation, without being toxic as depicted by white blood cell count [3]. Clinical indications: Abdominal abscess; Acute bronchitis; Acute sinusitis; Bacterial infectionToxicity: Symptoms of overdose include CNS and gastrointestinal effects such as decreased activity, somnolence, tremor, convulsions, vomiting, and diarrhea. The minimal lethal intravenous dose in mice and rats is 100 mg/kg.
RNPA1000 is an attractive antimicrobial development candidate; RnpA inhibitor.IC50 value:Target: RnpA inhibitorThe antibiotic vancomycin and a novel Staphylococcus aureus RnpA inhibitor under pre-clinical development, RNPA1000, were included in these studies. Rheological testing characterized the workability of the glass polyalkenoate cement over a range of powder-to-liquid ratios and polyacrylic acid concentrations and revealed that the most suitable powder-to-liquid ratio was 2/1.25 with 40 wt% polyacrylic acid. Loading glass polyalkenoate cement with either 20-30% RNPA1000 or vancomycin prevented bacterial growth. However, longer incubations allowed for Staphylococcus aureus colonies to form near the vancomycin-infused cement, indicating that vancomycin may not be suitable for long-term biofilm inhibition in comparison to RNPA1000.
MmpL3-IN-3 (Compound 12) is a MmpL3 inhibitor. MmpL3-IN-3 shows a MIC of 0.1 μM against H37Rv. MmpL3-IN-3 shows good stability in mouse liver microsomes. MmpL3-IN-3 can be used for anti-tubercular research[1].
Lincomycin hydrochloride monohydrate is a narrow-spectrum antibiotic, has similar effects to erythromycin, which has a good effect on gram-positive coccus, mainly used to inhibit the synthesis of bacterial cell protein.
Phytolaccagenin, a triterpenoid saponin, is the active component of Radix Phytolaccae. Phytolcaccagenin has antifungal activity, anti-inflammatory activity and lower toxicity[1]
Isoastilbin is a dihydroflavonol glycoside compound in Rhizoma Smilacis glabrae and Astragalus membranaceus. Isoastilbin inhibits glucosyltransferase (GTase) with an IC50 value of 54.3 μg/mL, and also inhibits tyrosinase activity. Isoastilbin shows neuroprotective, antioxidation, antimicrobial and anti-apoptotic properties and has the potential for Alzheimer’s disease research[1][21][3].
Procyanidin A2 is a flavonoid found in cranberries and lingonberries, with anti-cancer, antioxidant, antimicrobial and anti-inflammation activity[1][2].
(±)-Emodin bianthrone (compound 10), a natural product, exhibits antimalarial, antitubercular and ntifungal activities[1].
HBV-IN-12 is a potent hepatitis B surface antigen (HBsAg) inhibitor (0.001 μM< EC50 ≤0.05 μM). HBV-IN-12 shows anti-HBV DNA activity (0.001 μM＜EC50 ≤0.02 μM). From patent WO2021204252A1, compound 15[1].
Lumefantrine D18 is the deuterium labeled Lumefantrine, which is an antimalarial drug.
Ceftizoxime is a bacterial inhibitor which acts by interfering with bacterial cell wall synthesis and inhibiting cross-linking of the peptidoglycan.
Azomycin is an antibiotic which can be active against aerobic Gram-positive and Gram-negative bacteria.
Bis(dihydrochelerythrinyl)amine possesses anti-bacteria activity[1].
Desaminotyrosine is a microbially associated metabolite protecting from influenza through augmentation of type I interferon signaling.
Claficapavir (A1752) is a specific nucleocapsid protein (NC) inhibitor with an IC50 around 1 μM. Claficapavir strongly binds the HIV-1 NC (Kd=20 nM) thereby inhibiting the chaperone properties of NC and leading to good antiviral activity against the HIV-1[1].
Streptomycin sulfate is an aminoglycoside antibiotic, that inhibits protein synthesis.
DS86760016 is a novel selective bacterial leucyl-tRNA synthetase (LeuRS) inhibitor with IC50 of 0.38 uM (Escherichia coli, LeuRS); inhibits Pseudomonas aeruginosa and Acinetobacter baumannii with IC50 of 0.62 and 0.16 uM, respectively; shows active against MDR Gram-negative bacteria (MIC 0.25-2 ug/mL) with an improved pharmacokinetic profile compared with GSK2251052; also shows lower mutant prevention concentrations against P. aeruginosa compared to GSK2251052.
Fosfomycin tromethamine (MK-0955 tromethamine) is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin tromethamine shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria[1].
Motavizumab (MEDI-524) is an anti-human RSV (respiratory syncytial virus) monoclonal antibody. Motavizumab can be used in respiratory syncytial virus infection in high-risk infants research[1].
Helioxanthin derivative 5-4-2 is an analogue of helioxanthin, exhibites significant in vitro anti-HBV activity with EC50 of 0.08 uM in HepG2.2.15 cells.IC50 value: 0.08 uM (EC50) [1][2]Target: Anti-HBVHelioxanthin derivative 5-4-2 had potent anti-HBV activities in HepG2.2.15 cells, with the EC50s of 1 and 0.08 microM, respectively. The lamivudine-resistant HBV, L526M/M550V double mutant strain, was also sensitive to helioxanthin and 5-4-2. This class of compounds not only inhibited HBV DNA, but also decreased HBV mRNA and HBV protein expression. The EC50 of HBV DNA inhibition was consistent with the EC50 of HBV 3.5 Kb transcript inhibition, which was 1 and 0.09 microM for helioxanthin and 5-4-2 respectively.
2,6-Dichlorodiphenylamine is an analogue of Diclofenac Sodium (HY-15037) and has anti-Candida albicans activity. Diclofenac Sodium is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells.
Amorolfine hydrochloride is a antifungal reagent.Target: AntifungalAmorolfine is an antifungal showing activity against fungi pathogenic to plants, animals and humans. Amorolfine possesses a broad antifungal spectrum including dermatophytes, yeasts, dimorphic fungi and moulds and is not only fungistatic but fungicidal against most species [1]. At 0.2, 2 and 5 micrograms/ml amorolfine did not have any significant inhibitory or enhancing effect on phagocytosis whether following simultaneous addition of blastospores and drug to the neutrophils, prior treatment of neutrophils for 2 h before addition of blastospores or prior treatment of blastospores for 2 h. Simultaneous addition of amorolfine resulted in a significant increase in killing at all concentrations. This increase was not significantly enhanced by either preincubation of neutrophils or blastospores for 2 h with the drug [2].
Tedizolid is a novel oxazolidinone, acting through inhibition of bacterial protein synthesis by binding to 23S ribosomal RNA (rRNA) of the 50S subunit of the ribosome.
Taurolidine is a broad-spectrum antimicrobial for the prevention of central venous catheter-related infections. Taurolidine has a direct and selective antineoplastic effect on brain tumor cells by the induction of apoptosis[1].
Methylisothiazolinone-d3 (hydrochloride) is the deuterium labeled Methylisothiazolinone (hydrochloride). 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.
PA (224-233), Influenza is a 10-aa peptide, a fragment of polymerase 2 protein in influenza A virus.
Bebtelovimab a humanized IgG1-λ2 antibody targeting to SARS-CoV-2, especially COVID-19. Bebtelovimab potently neutralizes SARS-CoV-2 variants, and inhibits COVID-19 with mild-to-moderate efficacy[1][2].
AcrB-IN-1 (Compound H6) is a potent AcrB inhibitor. AcrB-IN-1 can be used for the reversal of bacterial multidrug resistance[1].
NAG-thiazoline is a O-GlcNAcase inhibitor with a Ki of 180 nM. NAG-thiazoline is a potent GH20 GlcNAcase (VhGlcNAcase) inhibitor with an IC50 of 11.9 μM and a Ki of 62 µM[1].
SABA1 possesses antibacterial properties against Pseudomonas aeruginosa and Escherichia coli, with an IC50 of 4.0 µM against E. coli ACC[1].