Sanfetrinem (GV104326) sodium is a beta-lactamase-stable antibiotic. Sanfetrinem sodium has broad-spectrum activity against gram-positive and gram-negative bacteria[1].
Oleanolic aldehyde is an antimicrobial compound used to inhibit oral bacteria. Oleanolic aldehyde inhibits Streptococcus mutans and Porphyromonas gingivalis, which are associated with dental caries and periodontal disease, with minimum inhibitory concentrations (MICs) of 488 μg/mL and 250 μg/mL, respectively[1].
Braco-19 is a potent telomerase/telomere inhibitor, preventing the capping and catalytic action of telomerase. Braco-19 acts as G-quadruplex (GQ) binding ligand, stabilizing G-quadruplexes formation at the 3V telomeric DNA overhang and produce rapid senescence or selective cell death. Braco-19 is also a HAdV virus replication inhibitor[1][2].
Ivermectin B1a, a derivative of Avermectin B1a (HY-15308), is a main component of Ivermectin (HY-15310)[1]. Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19[2].
Antifungal agent 24 (Compound 6) is an antifungal agent against Candida albicans with a MIC value of 0.03 μg/mL[1].
Antibacterial agent 31 shows the antibacterial activity against rice bacterial leaf streak.
Mafenide Acetate is a sulfonamide-type medication.Target: OthersMafenide is a sulfonamide-type medication. Mafenide works by reducing the bacterial population present in the avascular tissues of burns and permits spontaneous healing of deep partial-thickness burns. It is used to treat severe burns. It is used topically as an adjunctive therapy for second- and third-degree burns. It is bacteriostatic against many gram-positive and gram-negative organisms, including Pseudomonas aeruginosa. Some sources state that mafenide is more appropriate for non-facial burns, while chloramphenicol/prednisolone or bacitracin are more appropriate for facial burns [1-3].
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.
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.
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].
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.
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.
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].
PA (224-233), Influenza is a 10-aa peptide, a fragment of polymerase 2 protein in influenza A virus.
AcrB-IN-1 (Compound H6) is a potent AcrB inhibitor. AcrB-IN-1 can be used for the reversal of bacterial multidrug resistance[1].
SABA1 possesses antibacterial properties against Pseudomonas aeruginosa and Escherichia coli, with an IC50 of 4.0 µM against E. coli ACC[1].
Fusidic acid (Fusidate) is a bacteriostatic antibiotic[1][2][3].
Vitamin D3-d3 is the deuterium labeled Vitamin D3. Vitamin D3 (Cholecalciferol; Colecalciferol) is a naturally occuring form of vitamin D. Vitamin D3 induces cell differentiation and prevents proliferation of cancer cells.
Urease is produced by many types of bacteria and is an effective virulence factor for some pathogenic bacteria. Urease is also central to the metabolism and virulence of Helicobacter pylori, helping it colonize the stomach lining[1].
Isoliquiritin, isolated from Licorice Root, inhibits angiogenesis and tube formation. Isoliquiritin also exhibits antidepressant-like effects and antifungal activity[1][2][3].