antibacterial action

Sulfisoxazole acetyl (Gantrisin) is an agent with antibacterial activity. Sulfisoxazole acetyl is a Sulfisoxazole derivative with antibacterial activity. Sulfisoxazole acetyl is an inhibitor of dihydropteroate synthase.

Antimicrobial agent-22 (THI 6c) is a broad-spectrum, multi-target antibacterial with rapid bactericidal efficacy, effective anti-biofilm activity, and low cytotoxicity and hemolytic properties [1].

Chloroxine (Capitrol) is a synthetic quinoline derivative with antibacterial activity. Although the mechanism of action is not fully understood, topical administration of chloroxine diminishes mitotic activity in the epidermis, thereby reducing excessive scaling associated with dandruff or seborrheic dermatitis of the scalp, including psoriasis and eczema.

Trimethoprim (NSC-106568) is a Dihydrofolate Reductase Inhibitor Antibacterial. The mechanism of action of trimethoprim is as a Dihydrofolate Reductase Inhibitor, and Cytochrome P450 2C8 Inhibitor, and Organic Cation Transporter 2 Inhibitor.

Ethionamide (2-ethylthioisonicotinamide) is a nicotinamide derivative, with antibacterial activity, used to treat tuberculosis. Although the exact mechanism of action of ethionamide is unknown, it may inhibit the synthesis of mycolic acid, a saturated fatty acid found in the bacterial cell wall, thereby inhibiting bacterial cell wall synthesis. This eventually leads to bacterial cell wall disruption and cell lysis. Ethionamide may be bacteriostatic or bactericidal in action, depending on the concentration of the drug at the site of infection and the susceptibility of the organism involved.

Ciclopirox (HOE296b) exerts its action by binding to and chelating trivalent cations, such as Fe3+ and Al3+, thereby inhibiting the availability of essential co-factors for enzymes. Ciclopirox is a synthetic, broad-spectrum antifungal agent with additional antibacterial and anti-inflammatory activities. This may lead to a loss of activity of enzymes that are essential for cellular metabolism, the organization of cell wall structure and other crucial cell functions. In addition, ciclopirox exerts its anti-inflammatory activity by inhibiting 5-lipoxygenase and cyclooxygenase (COX).

Erythromycin estolate is a semi-synthetic derivative of erythromycin with good oral absorption and bioavailability tolerance. As a macrolide antibiotic, Erythromycin exerts its antibacterial action by inhibiting bacterial protein synthesis and is mainly used in studies for the treatment of respiratory, skin and soft tissue infections caused by susceptible bacteria. Erythromycin estolate may cause liver injury, including mild cholestatic hepatitis, jaundice, and paucity of bile ducts.

Levofloxacin Hydrochloride Impurity A I, one of the quinolones, has a broad spectrum of antibacterial action.

Tazobactam (YTR-830H) is an antibacterial penicillin derivative which inhibits the action of bacterial beta-lactamases.

AVX 13616, Avexa's leading antibacterial candidate, demonstrates significant in vivo antibacterial efficacy, especially against drug-resistant Staphylococcus pathogens, with an IC50 value of 2-4 µg/ml (MICs) and is targeted as an antibacterial agent. Comparable in activity to mupirocin within a nasal decolonization model, AVX13616 necessitated only a single application for effectiveness. This compound, alongside others, exhibited broad-spectrum antibacterial action, achieving MICs of 2-4 micrograms per milliliter against various isolates, including S. aureus, coagulase-negative staphylococci, enterococci, MRSA, VISA, and VRSA. Aimed for topical use and the treatment of wound infection or catheter-related infections, a solitary 5% (w/w) AVX13616 application (roughly equivalent to 2% mupirocin) proved as efficacious as twice-daily 2% mupirocin over five days in decolonizing MRSA in mice.

Antibacterialagent 244 is a compound that exhibits broad-spectrum antibacterial activity and oral efficacy, primarily targeting Gram-positive bacteria with a minimum inhibitory concentration (MIC) of 1-4 μg mL. It possesses low hemolytic toxicity (HC50 of 111.6 μg mL). The mode of action for Antibacterialagent 244 involves disrupting the bacterial transmembrane potential and increasing membrane permeability, which leads to the leakage of cellular contents such as DNA and proteins, ultimately causing bacterial death. This compound is useful in research related to infections caused by Gram-positive bacteria.

Cefamandole is a broad-spectrum cephalosporin antibiotic with antibacterial activity against Bacillus subtilis and Escherichia coli.

Antibacterialagent 119 (Compound 21 g) is a potential antibacterial agent effective against methicillin-resistant Staphylococcus aureus, with a minimum inhibitory concentration (MIC) of less than 1 μg mL against tested strains. It induces reactive oxygen species (ROS) generation and disrupts bacterial cell membranes, causing their rupture. Antibacterialagent 119 exhibits strong antimicrobial activity, low cytotoxicity, rapid bactericidal action, and favorable in vivo antibacterial efficacy.

Ro 24-4383 is a dual-action antibacterial agent linked by carbamate.

Ro-23-9424 is a dual-action cephalosporin with a fleroxacin esterified at the 3' position and aminothiazolylmethoxyimino-type side chain at the 7 position. Ro-23-9424 has broad and potent antibacterial activity in vitro and in vivo.

Flumequine-13C3is intended for use as an internal standard for the quantification of flumequine by GC- or LC-MS. Flumequine is a fluoroquinolone antibiotic.1It is active againstS. aureus, S. pyogenes, B. subtilis, E. coli, P. aeruginosa, S. faecalis, andK. pneumoniae(MICs = 1-100 μg/ml). Flumequine is also active against field isolates of B. hyodysenteriae (MICs = 6.25-200 μg/ml).2It inhibits DNA gyrase, disrupting supercoiling of bacterial DNA to block transcription and replication.3In vivo, flumequine (50 mg/kg) increases survival in rat models ofP. vulgaris-induced urinary tract infection andP. mirabilis-induced prostatitis.1Formulations containing flumequine have been used in the treatment of urinary tract infections in veterinary medicine. 1.Rohlfing, S.R., Gerster, J.R., and Kvam, D.C.Bioevaluation of the antibacterial flumequine for urinary tract useAntimicrob. Agents Chemother.10(1)20-24(1976) 2.Aller-Morán, L.M., Martínez-Lobo, F.J., Rubio, P., et al.Evaluation of the in vitro activity of flumequine against field isolates of Brachyspira hyodysenteriaeRes. Vet. Sci.10351-53(2015) 3.Smith, J.T.The mode of action of 4-quinolones and possible mechanisms of resistanceJ. Antimicrob. Chemother.18 (Suppl. D)21-29(1986)

3-O-Methylgalangin (GALANGIN-3-METHYLETHER) has antibacterial activity, it has inhibitory effects on Pseudomonas aeruginosa. GALANGIN-3-METHYLETHER has hypolipidemic activity, the action is due to the inhibition of pancreatic lipase.

Antibacterial agent 94 (compound 5b) is a highly effective antibacterial agent demonstrating strong activity against various bacterial strains, notably eradicating MRSA persisters and highlighting its therapeutic potential. Its mechanism of action involves interference with the bacterial membrane and disruption of the phosphatidylglycerol (PG) synthesis pathway [1].

Antibacterial agent 110 (Compound 4e) is a potent antibacterial agent effective against P. aeruginosa (MIC: 1 μg ml), disrupting cell membranes and exhibiting strong antibacterial membrane activity.

Parconazole Free Base is used in veterinary as an oral fungicide with a broad-spectrum activity against dermatophytes, yeasts, and others fungi. This compound does not have any antibacterial effect. The mechanism of action involves inhibition of the fungal cytochrome P450 dependent 14alpha-dimethylation of lanosterol to ergosterol.

Ethionamide HCl is the salt form of Ethionamide, a second-line antitubercular agent that inhibits mycolic acid synthesis. Ethionamide is a nicotinamide derivative, with antibacterial activity, used to treat tuberculosis. Although the exact mechanism of action of ethionamide is unknown, it may inhibit the synthesis of mycolic acid, a saturated fatty acid found in the bacterial cell wall, thereby inhibiting bacterial cell wall synthesis. This eventually leads to bacterial cell wall disruption and cell lysis. Ethionamide may be bacteriostatic or bactericidal in action, depending on the concentration of the drug at the site of infection and the susceptibility of the organism involved. It binds with NAD+ to form an adduct.

FtsZ-IN-7 is a potent inhibitor of FtsZ, promoting FtsZ polymerization while inhibiting its GTPase activity, which disrupts bacterial cell division and leads to bacterial cell death. It shows bactericidal effects without significant bacterial resistance, exhibits rapid antibacterial action, and has minimal hemolytic activity and cytotoxicity towards mammalian cells [1].

Pazufloxacin (T-3761) is a fluoroquinolone antibiotic used for antibacterial applications. This novel quinolone derivative exhibits robust and broad-spectrum antibacterial efficacy against systemic, pulmonary, and urinary tract infections in mice, effectively targeting both gram-positive and gram-negative bacteria, including quinolone-resistant strains such as Serratia marcescens and Pseudomonas aeruginosa. Compared to antibiotics like ofloxacin, ciprofloxacin, norfloxacin, and tosufloxacin, Pazufloxacin demonstrates comparable or superior efficacy across various infection models. While slightly less effective than tosufloxacin against certain gram-positive infections, it remains potent against methicillin-resistant Staphylococcus aureus. Its broad-spectrum activity is supported by minimum inhibitory concentrations (MICs) between 0.39 and 6.25 micrograms/ml for Staphylococcus aureus and Clostridium species, with minimum bactericidal concentrations (MBCs) close to the MICs. Additionally, its 50% inhibitory concentrations for DNA gyrases from E. coli and P. aeruginosa are 0.88 and 1.9 micrograms/ml respectively, highlighting its potent antibacterial mechanism of action.

Batzelladine D, also known as Compound 1, functions as an inhibitor of the Pdr5p transporter's catalytic and functional activities, demonstrating inhibitory action against Pdr5p ATPase activity with an IC50 value of 7.1 µM. Additionally, it exhibits a range of bioactivities including antifungal, antiparasitic, antiviral, antibacterial, and antitumoral properties [1].