Antibacterial agent 108 (Compound 1h) is a potent antibacterial agent with a MIC of both 3 μM against MRSA and antibiotic resistance strains[1].
Bacampicillin hydrochloride is a penicillin antibiotic, is a prodrug of ampicillin with improved oral bioavailability.
Sulbactam(Betamaze) is an irreversible β-lactamase inhibitor.Target: β-lactamase; AntibacterialSulbactam is a mechanism-based inhibitor of beta-lactamase enzymes used in clinical practice. sulbactam was the antimicrobial agent responsible for the killing of these organisms [1]. sulbactam may prove effective for non-life-threatening A. baumannii infections. Its role in the treatment of severe infections is unknown. However, the current formulation of sulbactam alone may allow its use at higher doses and provide new potential synergic combinations, particularly for those infections by A. baumannii resistant to imipenem [2].
Cyclo(L-Trp-L-Trp) is an antibiotic, and shows antimicrobial activity. Cyclo(L-Trp-L-Trp) can inhibit A. baumannii, as well as Candida albicans, Bacillus subtilis, Micrococcus luteus, Saccharomyces cerevisiae, Aspergillus niger, Staphylococcus aureus. Cyclo(L-Trp-L-Trp) can be used in microbial infection research[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.
Bis(dihydrochelerythrinyl)amine possesses anti-bacteria activity[1].
Streptomycin sulfate is an aminoglycoside antibiotic, that inhibits protein synthesis.
AcrB-IN-1 (Compound H6) is a potent AcrB inhibitor. AcrB-IN-1 can be used for the reversal of bacterial multidrug resistance[1].
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].
Ethambutol is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases.Target: AntibacterialEthambutol directly affects two polymers, arabinogalactan (AG) and lipoarabinomannan (LAM) in Mycobacterium smegmatis. In M. smegmatis, Ethambutol inhibits synthesis of arabinan completely and inhibits AG synthesis most likely as a consequence of this; more than 50% of the cell arabinan is released from the bacteria following Ethambutol treatment, whereas no galactan is released. Ethambutol main targets against embB gene product in M. avium. Ethambutol induces 60% changes in the embB gene in M. tuberculosis resistant mutants [1]. Ethambutol is effective against actively growing microorganisms of the genus Mycobacterium, including M. tuberculosis. Nearly all strains of M. tuberculosis and M. kansasii as well as a number of strains of the M. aviumcomplex (MAC) are sensitive to Ethambutol. [1] Ethambutol is potency against M. tuberculosis (H37Rv) with MIC of 0.5 μg/mL in vitro [2]. Ethambutol is efficient on treatment of mycobacterial-infected macrophages. When M. tuberculosis infected macrophages are treated with 6 μg/mL Ethambutol, the log CFUs following treatment for 3 days is 4.17, while value in control group is 4.8. The MICs for M. avium (MTCC 1723) and M. smegmatis (MTCC 6) are 15 μg/mL and 0.18 μg/mL, respectively. Ethambutol is efficient in animal model. 100 mg/kg Ethambutol given orally 15 days post i.v. infection 1 ×/week for 5 weeks, induces a lower log CFU compared with untreatment (4.59 vs 5.07) [3].
Polymyxin B nonapeptide TFA is a cyclic peptide obtained from Polymyxin B by proteolytic removal of its terminal amino acyl residue[1]. Polymyxin B nonapeptide TFA is less toxic, lacks bactericidal activity, and retains its ability to render gram-negative bacteria susceptible to several antibiotics by permeabilizing their outer membranes[2].
Bio-AMS is a chemical inhibitor of Mycobacterium tuberculosis biotin protein ligase ( MtBPL) with Kd of 0.865 nM; possesses selective activity against Mycobacterium tuberculosis ( Mtb) and arrests fatty acid and lipid biosynthesis, enhances tuberculosis chemotherapy (rifampicin and ethambutol).
1-Tetradecanol, isolated from Myristica fragrans, is a straight-chain saturated fatty alcohol. 1-Tetradecanol possesses antibacterial and anti-inflammatory (periodontitis) activity[1].
D-Ribonolactone is sugar lactone and an inhibitor of β-galactosidase of Escherichia coli with a Ki of 26 mM[1].
(+)-Thienamycin is a potent broad-spectrum antibacterial and β-lactamase inhibitor that can be from Streptomyces cattleya[1].
4-Aminosalicylic acid (ASA) is an orally active antibiotic and has the potential to treat tuberculosis[1].
2-Chloroacetamide is a preservative and is a herbicide for both uplands and paddy fields. 2-Chloroacetamide is a biocide in agriculture, glues, paints and coatings. 2-Chloroacetamide inhibits very-long-chain fatty acid elongase[1][2][3].
Nalidixic acid sodium salt, a quinolone antibiotic, is effective against both gram-positive and gram-negative bacteria. Nalidixic acid acts in a bacteriostatic manner in lower concentrations and is bactericidal in higher concentrations. Nalidixic acid inhibits a subunit of DNA gyrase and topoisomerase IV and reversibly blocks DNA replication in susceptible bacteria[1][2].
Iseganan is an antimicrobial peptide, shows broad-spectrum anti-bacteria and fungi activity. Iseganan can be used in oral mucositis research[1][2][3].
GSK2200150A, identified by high-throughput screening (HTS) campaign, is an anti-tuberculosis (TB) agent.
DNA Gyrase-IN-2 (Compound 22a) is a bacterial DNA gyrase B inhibitor with IC50s of 3.29-10.49 and 4.41-5.61 µM for E. coli DNA gyrase and M. tuberculosis DNA gyrase. Anti-tubercular and antibacterial activity[1].
Zabofloxacin hydrochloride (DW-224a) is a novel fluoronaphthyridone quinolone that is considered a potent antibacterial candidate for clinical trials.Zabofloxacin hydrochloride (DW-224a) has excellent activity against gram-positive pathogens including Steptococcus aureus (S. aureus), Streptococcus pyogenes (S. pyrigenes), and S. pneumonia.Zabofloxacin hydrochloride (DW-224a) is considered as an alternative candidate for treatment of quinolone-susceptible (QSSP) and quinolone-resistant gonorrhea (QRSP)[1].
Dermaseptin-B3 inhibits the growth of Gram-positive and Gram-negative bacteria (MIC: 1.3, 2.3, 5.0, 2.6, 2.3 μM for S. aureus, P. aeruginosa, P. aeruginosa, E. (ATCC 25922), E. (54127) respectively). Dermaseptin-B3 also inhibits tumor cell proliferation[1][2].
Acridone is an organic compound based on the acridine skeleton. Acridone has antibacterial, antimalarial, antiviral and anti neoplastic activities[1].
Amikacin hydrate (BAY 41-6551 hydrate), a semisynthetic analog of kanamycin, is very active against most gram-negative bacteria including gentamicin- and tobramycin-resistant strains. Amikacin hydrate (BAY 41-6551 hydrate) is ototoxic and nephrotoxic[1][2].