2,4-Diacetylphloroglucinol, produced by some isolates of the beneficial bacterium Pseudomonas fluorescens, is a potent antibiotic. 2,4-Diacetylphloroglucinol is active against numerous organisms, including plants, fungi, viruses, bacteria, and nematodes[1].
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].
Desacetylcephapirin sodium (Deacetylcephapirin sodium) is an active metabolite of Cephapirin (HY-A0153A). Desacetylcephapirin sodium has antimicrobial against S. aureus and coagulase-negative staphylococci mastitis pathogen[1][2].
Dalbavancin-d6 is the deuterium labeled Dalbavancin[1]. Dalbavancin (MDL-63397) is a semisynthetic lipoglycopeptide antibiotic with potent bactericidal activity against Gram-positive bacteria. Dalbavancin inhibits Staphylococcus aureus and Bacillus anthracis with MIC90s of 0.06 μg/mL and 0.25 μg/mL, respectively[2][3].
Sulfadiazine D4 is a deuterium labeled Sulfadiazine. Sulfadiazine is a sulfonamide antibiotic used for the treatment of toxoplasmosis[1][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].
Ciprofloxacin (Bay-09867) lactate is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin lactate induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin lactate has anti-proliferative activity and induces apoptosis. Ciprofloxacin lactate is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity[1][2][3][4].
ACHN-975 is a selective LpxC inhibitor, exhibiting a subnanomolar LpxC inhibitory activity and low MIC values (≤1 μg/mL) against a wide range of Gram-negative bacteria. LpxC is highly conserved in Gram-negative bacteria and catalyzes the first committed step of lipid A biosynthesis[1]. LpxC is the bacterial enzyme Zinc-dependent metalloamidase UDP-3-O-[(R)-3-hydroxymyristoyl]-N-acetylglucosamine deacetylase[1].
Tigecycline hydrate is a broad spectrum glycylcycline antibiotic. Tigecycline hydrate is bacteriostatic, that inhibits protein synthesis by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation. Tigecycline hydrate is active against resistant strains of Gram-positive and Gram-negative bacteria.
Lindenenol is isolated from Radix linderae, with antioxidant and antibacterial activities[1].
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].
Imidazolidinyl urea is an antimicrobial preservative used in cosmetics, acts as a formaldehyde releaser.
Avarofloxacin (JNJ-Q2) is a broad-spectrum fluoroquinolone antibacterial drug being developed for the treatment of acute bacterial skin and skin-structure infections and community-acquired pneumonia[1]. Avarofloxacin (JNJ-Q2) is an aminoethylidenylpiperidine fluoroquinolone that demonstrates antibacterial effect against numerous Gram-positive bacteria with a mean 0.12 mg/L MIC90 value[2]. Avarofloxacin (JNJ-Q2) has potential for treatment of methicillin-resistant Staphylococcus aureus (MRSA) infections[3].
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.
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].
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].
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].