bacterial infection

Bithionol (Actamer), formerly marketed as an active ingredient in various topical drug products, was shown to be a potent photosensitizer with the potential to cause serious skin disorders. Approvals of the NDA's for bithionol drug products were withdrawn on October 24, 1967.

Rifaximin is an orally administered, semi-synthetic, nonsystemic antibiotic derived from rifamycin SV with antibacterial activity. Rifaximin binds to the beta-subunit of bacterial DNA-dependent RNA polymerase, inhibiting bacterial RNA synthesis and bacter

Sulfameter (Sulfametoxydiazine) is a long-acting sulfonamide antibacterial agent used to treat urinary tract infections and leprosy.

Ceftazidime (GR20263) is a beta-lactam, cephalosporin antibiotic with bactericidal activity.

Tridecanoic acid (Tridecylic Acid) is a 13-carbon saturated fatty acid found in dairy products and also as a product of anaerobic biodegradation of n-hexadecane. It has been identified as a substrate of phospholipase A2.

3,4,5-Trimethoxybenzaldehyde shows anti-Candida efficacy and inhibits adhesion and biofilms.

Sitafloxacin Hydrate (DU-6859a) is a fluoroquinolone antibiotic that shows promise in the treatment of Buruli ulcer.

Acetylspiramycin (Spiramycin B) targets 50S ribosome to inhibit protein synthesis.

Metronidazole (Metronidazol) is a synthetic nitroimidazole derivative with antiprotozoal and antibacterial activities.

Sulfamethoxazole sodium (Ro 4-2130 sodium) is a sulfonamide bacteriostatic antibiotic.

Cefmetazole sodium (Sodium cefmetazole) is a semisynthetic cephamycin antibiotic with broad-spectrum activity against both gram-positive and gram-negative microorganisms. It demonstrates a high rate of efficacy in various types of infections, and to date, no severe side effects have been noted.

Nitrofurantoin (Furadantine), an antibiotic, inhibits bacterial DNA, RNA, and cell wall protein synthesis. Activated by bacterial flavoproteins to intermediates that inactivate bacterial ribosomal proteins, Nitrofurantoin is used prophylactically as a urinary anti-infective agent against most gram-positive and gram-negative organisms and for long-term suppression of infections.

Imipenem monohydrate (Imipenem) is a carbapenem antibiotic isolated from the microorganism Streptomyces cattleya, and is a β lactam antibiotic. Imipenem monohydrate acts on the bacterial cell wall, and is a broadly effective inhibitor of a wide range of Gram-positive and negative bacteria.

Hexetidine (NSC-17764) is a bactericidal and fungicidal antiseptic. It is used as a 0.1% mouthwash for local infections and oral hygiene.

Paromomycin binds specifically to the RNA oligonucleotide at the A site of bacterial 30S ribosomes, thereby causing misreading and premature termination of translation of mRNA and inhibition of protein synthesis followed by cell death. Paromomycin Sulfate (Aminosidine sulfate) is the sulfate salt form of paromomycin, a structural derivative of neomycin, an aminoglycoside antibiotic with amebicidal and bactericidal effects against predominantly aerobic gram-negative bacteria.

N-acetyl Sulfamethoxazole is a metabolite of sulfamethoxazole, an antibiotic with antiviral activity, that can be detected in urine.

Minocycline hydrochloride (Minocycline HCl) is a tetracycline antibiotic with excellent absorption and tissue penetration that is used for several bacterial infections as well as treatment of acne. Minocycline hydrochloride can cause both an acute hepatitis-like syndrome occurring within 1 to 3 months of starting therapy or a more insidious chronic hepatitis with autoimmune features typically after long-term treatment.

Silver sulfadiazine (Dermazin) is a sulfonamide-based topical agent with antibacterial and antifungal activity.

Lomefloxacin hydrochloride (Okacyn) inhibits DNA gyrase, a type II topoisomerase involved in the induction or relaxation of supercoiling during DNA replication. This inhibition leads to a decrease in DNA synthesis during bacterial replication, resulting in cell growth inhibition and eventually cell lysis. Lomefloxacin Hydrochloride is the hydrochloride salt form of lomefloxacin, a synthetic broad-spectrum fluoroquinolone with antibacterial activity.

Novobiocin Sodium (Albamycinsodium) binds to DNA gyrase and blocks adenosine triphosphatase (ATPase) activity. Novobiocin sodium is an antibiotic compound derived from Streptomyces niveus. It has a chemical structure similar to coumarin.

Ronidazole (Ronidazol) is an antiprotozoal and antimicrobial agent used mainly in veterinary practice.

Methicillin sodium salt is the sodium salt form of methicillin, a semisynthetic beta-lactam penicillin antibiotic with beta-lactamase resistant activity.

Glyceryl monocaprate (2,3-Dihydroxypropyl decanoate) has inhibitory effect on Herpes Simplex Virus (HSV). It also offers an effective treatment for herpes labialiss. Glyceryl monocaprate is a capric acid against 1-monoglyceride gram-positive bacterial infections.

Mezlocillin Sodium (Baycipen) is a penicillin beta-lactam antibiotic used in the treatment of bacterial infections caused by susceptible, usually gram-positive, organisms.

Cefazolin-13C2,15N is intended for use as an internal standard for the quantification of cefazolin by GC- or LC-MS. Cefazolin is a broad-spectrum cephalosporin antibiotic that is active in vitro against various Gram-positive and Gram-negative bacteria (MICs = 0.2-12.5 μg/ml). It also inhibits the growth of clinical isolates of S. aureus, E. coli, P. mirabilis, and K. pneumoniae (MICs = 0.1-25 μg/ml). In vivo, cefazolin protects against S. aureus, E. coli, and P. mirabilis infection in mice (ED50s = <0.09-1.78, 0.44-3.63, and 2.31-5.2 mg/animal, respectively). Formulations containing cefazolin have been used to treat a variety of bacterial infections.

YJ182 is an NDM-1 inhibitor with an IC50 of 0.23 μM, and additionally inhibits IMP-1, VIM-2, GIM-1, and MMP-2 with respective IC50 values of 0.25, 0.61, 0.49, and 6.92 μM. It is utilized in bacterial infection research [1].

Cefazolin sodium pentahydrate, a first-generation cephalosporin antibiotic, is employed in diverse bacterial infection research [1] and exhibits an anti-inflammatory effect capable of attenuating post-operative cognitive dysfunction (POCD) [2].

LmNADK1-IN-1 (compound MC1) is an inhibitor of nicotinamide adenine dinucleotide kinases (NADK1) from L. monocytogenes, with a K_i value of 54 nM, and can be used for bacterial infection research [1].

Ceftazidime Pentahydrate is a cephalosporin antibiotic with activity against gram-negative bacilli, including Pseudomonas aeruginosa, and is used in the study of infectious diseases.

Chloramphenicol palmitate is a broad-spectrum antibiotic with activity against gram-positive and gram-negative bacteria. Chloramphenicol palmitate can be used in studies about acting as a bacterial selection agent in transformed cells containing chloramphenicol resistance genes.

ANT3310 is an inhibitor of broad-spectrum covalent Serine β-Lactamase with IC50s ranging from 1 nM to 175 nM for AmpC, CTX-M-15, TEM-1, OXA-48, OXA-23, and KPC-2. ANT3310 can be used in studies about bacterial infection.

Doripenem is a broad-spectrum carbapenem antibiotic effective against both Gram-negative and Gram-positive bacteria, such as S. aureus, S. pneumoniae, E. coli, and K. pneumoniae, with minimum inhibitory concentrations (MICs) ranging from less than 0.015 to 0.3 µg/ml. It has been proven to reduce the viable bacteria count in mouse lung models of chronic P. aeruginosa respiratory tract infection at a dosage of 100 mg/kg per day. Doripenem operates by inhibiting bacterial cell wall synthesis through the formation of stable acyl-enzyme complexes with penicillin-binding proteins, leading to their inactivation. This compound has been utilized in various formulations for the treatment of bacterial infections.

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.

β-Lactamase-IN-2 is an inhibitor of β-Lactamase with anti-microbial and anti-bacterial effects.

(6E,12E)-Tetradecadiene-8,10-diyne-1,3-diol is an antibacterial compound isolated from the roots of Atractylodes japonica, exhibiting anti-methicillin-resistant Staphylococcus aureus (MRSA) activity with MIC values of 4-32 μg mL, and can be used for the research of bacterial infection [1].

Cefteram pivoxil (T-2588) (CFTM-PI) is an oral antibiotic available in powder suspension and tablet formulations indicated in China for the treatment of bacterial infections. 

OP-145, a derivative of the antimicrobial peptide LL-37, is a synthetic antimicrobial peptide showing activity against E. coli, P. aeruginosa, C. albicans, and A. niger, with minimum inhibitory concentrations (MICs) of 2, 3, 6, and 18 µM, respectively. Utilizing poly(lactic-co-glycolic acid) (PLGA) microspheres loaded with OP-145 effectively prevents biofilm formation in a mouse model of bone infection, which is initiated by surgical femoral fracture and subsequent bacterial inoculation at the fracture site.

Cefditoren-d3 is a deuterated compound of Cefditoren. Cefditoren has a CAS number of 104146-53-4. Cefditoren sodium is a cephalosporin antibiotic potentially for the treatment of bacterial infection. The expression levels of Mrp2, Bcrp, Oat2 mRNA were markedly increased, while P-gp and Oct1 mRNA were decreased. In concordance with RT-PCR results, Mrp2 expression level increased by Western blotting.

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.

Lenampicillin hydrochloride is an orally active prodrug of Ampicillin. Lenampicillin hydrochloride is an effective beta-lactam antibacterial agent that inhibits bacterial penicillin-binding proteins. It is applied in the investigation of suppurative skin

Dusquetide is a first-in-class innate defense regulator. Dusquetide displays activity in both reducing inflammation and increasing the clearance of bacterial infection.

Flurithromycin ((8S)-8-Fluoroerythromycin A) is an orally active, broad-spectrum antibiotic used in bacterial infection research [1] [2] [3].

Cefditoren sodium is a cephalosporin antibiotic potentially for the treatment of bacterial infection. The expression levels of Mrp2, Bcrp, Oat2 mRNA were markedly increased, while P-gp and Oct1 mRNA were decreased. In concordance with RT-PCR results, Mrp2

Dimethyldioctadecylammonium (DDA) is a cationic amphipathic lipid. DDA liposomes containing an Ag85B-ESAT-6 antigen induce antigen deposition at an intramuscular or subcutaneous injection site in mice, increasing immune cell exposure to the antigen. In a guinea pig model of M. tuberculosis infection, spleen bacterial load is reduced and lung and spleen lesion numbers are decreased when the mycobacterial lipid antigens Ac2SGL and PIM2 are administered in liposomes comprised of DDA and a synthetic analog of the mycobacterial cord factor trehalose 6,6-dibehenate (TDB). DDA has also been used in the study of lipid bilayer dynamics.

Ertapenem sodium (MK-826) is a new long-acting 1-β-methyl carbapenem antibiotic with a broad antibacterial spectrum including common aerobic and anaerobic bacteria and organisms with extended-spectrum β-lactamases.

H-Arg-OtBu (dihydrochloride) is a membrane-targeting antimicrobial that interacts with the negatively charged bacterial membrane through electrostatic and hydrophobic interactions, making it useful for bacterial infection disease research [1].

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)

Synthetic furanone bacterial quorum sensing inhibitor. Inhibits virulence factor expression in Pseudomonas aeruginosa and increases bacterial susceptibility to antibiotics in vitro. Also inhibits bacterial quorum sensing in vivo and promotes bacterial clearance in a mouse pulmonary infection model. Hentzer et al (2003) Attenuation of Pseudomonas aeruginosa virulence by quorum sensing inhibitors. EMBO J. 22 3803 PMID:12881415

Pap12-6, an antibacterial peptide originating from the first twelve N-terminal amino acids of papiliocin found in P. xuthus larvae, exhibits activity against a range of eight Gram-negative bacteria (e.g., E. coli, P. aeruginosa, S. syphimurium with MIC50s=4-8 µM) and Gram-positive bacteria (e.g., S. aureus, methicillin-resistant S. aureus 3126, B. subtilis, and S. epidermidis with MIC50s=4-8 µM), without compromising the viability of human erythrocytes, mouse RAW 264.7 macrophages, human HaCaT keratinocytes, or human HEK293 kidney cells at 25 µM. It causes membrane depolarization in E. coli at 4 and 8 µM and, upon preincubation at 10 µM, decreases nitrite (NO2-), Tnf-α, and Il-6 secretion in LPS-stimulated RAW 264.7 macrophages. In a murine model, Pap12-6 enhances survival rates and diminishes colony forming units (CFUs) in several organs upon E. coli infection at 10 mg/kg and 1 mg/kg doses, respectively. Additionally, at a 1 mg/kg dose, it lowers serum aspartate aminotransferase (AST) and alanine transaminase (ALT) levels, as well as blood urea nitrogen levels in E. coli-induced sepsis, indicating its therapeutic potential for bacterial infections without affecting host cell viability.

Monophosphoryl lipid A (MPLA) is a natural agonist for the toll-like receptor-4 (TLR4). It is useful as an adjuvant in immunization. MPLA is a safe prophylactic agent and has immunotherapeutic applications. It induces tumor necrosis factor and interleukin (IL)-1β, however not as efficient as lipopolysaccharide (LPS). MPLA improves immune response during bacterial sepsis infection.