U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 11 - 20 of 91 results

AG-205 was identified from high-throughput screening as a potent inhibitor of FabK, the enoyl-ACP reductase in Streptococcus pneumoniae. Specific inhibition of lipid biosynthesis in a macromolecular biosynthesis assay and identification of an Ala141Ser substitution in FabK from spontaneous AG205-resistant mutants indicated that AG-205 exerts antibacterial activity against S. pneumoniae through the specific inhibition of FabK. Small molecule AG-205 inhibits Pgrmc1 (Progesterone Receptor Membrane Component 1), a heme-1 domain protein that promotes tumorigenesis. AG-205 arrests growth in lung cancer cells.
Alatrofloxacin is a fluoroquinolone antibiotic developed as a mesylate salt and was sold under brand name Trovan, but was withdrawn from the U.S. market in 2001. Trovan was indicated for the treatment of patients initiating therapy in in-patient health care facilities (i.e., hospitals and long term nursing care facilities) with serious, life- or limb-threatening infections caused by susceptible strains of the designated microorganisms in the conditions listed below. Nosocomial pneumonia caused by Escherichia coli, Pseudomonas aeruginosa, Haemophilus influenzae, or Staphylococcus aureus. Community acquired pneumonia caused by Streptococcus pneumoniae, Haemophilus influenzae, Klebsiella pneumoniae, Staphylococcus aureus. Complicated intra-abdominal infections, including post-surgical infections caused by Escherichia coli. Gynecologic and pelvic infections including endomyometritis, parametritis, septic abortion and post-partum infections caused by Escherichia coli, Bacteroides fragilis, viridans group streptococci, Enterococcus faecalis. Complicated skin and skin structure infections, including diabetic foot infections, caused by Staphylococcus aureus, Streptococcus agalactiae, Pseudomonas aeruginosa, Enterococcus faecalis, Escherichia coli, or Proteus mirabilis. After intravenous administration, alatrofloxacin is rapidly converted to trovafloxacin, which is responsible for therapeutic effect. Plasma concentrations of alatrofloxacin are below quantifiable levels within 5 to 10 minutes of completion of a 1 hour infusion.
Netilmicin is a semisynthetic, water soluble antibiotic of the aminoglycoside group, produced by the fermentation of Micromonospora inyoensis, a species of actinomycete. Aminoglycosides are useful primarily in infections involving aerobic, Gram-negative bacteria, such as Pseudomonas, Acinetobacter, and Enterobacter. It is active at low concentrations against a wide variety of pathogenic bacteria including Escherichia coli, bacteria of the Klebsiella-Enterobacter-Serratia group, Citrobacter sp., Proteus sp. (indole-positive and indole-negative), including Proteus mirabilis, P. morganii, P. rettgrei, P. vulgaris, Pseudomonas aeruginosa and Neisseria gonorrhoea. Netilmicin is also active in vitro against isolates of Hemophilus influenzae, Salmonella sp., Shigella sp. and against penicillinase and non-penicillinase-producing Staphylococcus including methicillin-resistant strains. Some strains of Providencia sp., Acinetobacter sp. and Aeromonas sp. are also sensitive to netilmicin. Many strains of the above organisms which are found to be resistant to other aminoglycosides, such as kanamycin, gentamicin, tobramycin and sisomicin, are susceptible to netilmicin in vitro. Occasionally, strains have been identified which are resistant to amikacin but susceptible to netilmicin. The combination of netilmicin and penicillin G has a synergistic bactericidal effect against most strains of Streptococcus faecalis (enterococcus). The combined effect of netilmicin and carbenicillin or ticarcillin is synergistic for many strains of Pseudomonas aeruginosa. In addition, many isolates of Serratia, which are resistant to multiple antibiotics, are inhibited by synergistic combinations of netilmicin with carbenicillin, azlocillin, mezlocillin, cefamandole, cefotaxime or moxalactam. Netilmicin "irreversibly" binds to specific 30S-subunit proteins and 16S rRNA. Specifically netilmicin binds to four nucleotides of 16S rRNA and a single amino acid of protein S12. This interferes with decoding site in the vicinity of nucleotide 1400 in 16S rRNA of 30S subunit. This region interacts with the wobble base in the anticodon of tRNA. This leads to interference with the initiation complex, misreading of mRNA so incorrect amino acids are inserted into the polypeptide leading to nonfunctional or toxic peptides and the breakup of polysomes into nonfunctional monosomes, leaving the bacterium unable to synthesize proteins vital to its growth.
Bacampicillin is a penicillin antibiotic. It is a prodrug of ampicillin with improved oral bioavailability. It exerts bactericidal activity via inhibition of bacterial cell wall synthesis by binding one or more of the penicillin binding proteins (PBPs). Spectrobid is used to treat bacterial infections such as tonsillitis, pneumonia (lung infection), bronchitis (inflammation of airway), urinary tract infections, gonorrhea, and infections of the skin. Adverse effects are: anemia, thrombocytopenia, neutropenia, agranulocytosis, seizures, nephrotoxicity, Jarisch-Herxheimer Reaction (fever, chills, sweating, tachycardia, hyperventilation, flushing, and myalgia). Drug interactions: Contraceptives - decreased contraceptive effectiveness; Live Typhoid Vaccine - decreased immunological response to the typhoid vaccine; Probenecid - increased bacampicillin levels.
Status:
US Previously Marketed
Source:
Matromycin by Pfizer
(1956)
Source URL:
First approved in 1956
Source:
Matromycin by Pfizer
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Oleandomycin is a macrolide antibiotic, which was first described under the designation P.A.105 by Sobin, English, and Celmer (1954-5). Later it appeared on the market under three names and in two forms: as pure oleandomycin ("matromycin," Pfizer; "romicil," Hoffmann-La Roche) and as a mixture with twice its weight of tetracycline ("sigmamycin," Pfizer). Oleandomycin can be employed to inhibit the activities of bacteria responsible for causing infections in the upper respiratory tract much like Erythromycin can. Both can affect staphylococcus and enterococcus genera. Oleoandomycin is reported to inhibit most gram-positive bacteria, but has only a slight inhibiting effect on gram-negative bacteria, rickettsiae, and larger viruses. The spectrum of activity on micro-organisms is therefore wider than that of penicillin and streptomycin, but narrower than that of chloramphenicol and the tetracyclines. Oleandomycin is approved as a veterinary antibiotic in some countries. It has been approved as a swine and poultry antibiotic in the United States. However, it is currently only approved in the United States for production uses. Oleandomycin is a bacteriostatic agent. Like erythromycin, oleandomycin binds to the 50s subunit of bacterial ribosomes, inhibiting the completion of proteins vital to survival and replication. It interferes with translational activity but also with 50s subunit formation. However, unlike erythromycin and its effective synthetic derivatives, it lacks a 12-hydroxyl group and a 3-methoxy group. This change in structure may adversely affect its interactions with 50S structures and explain why it is a less powerful antibiotic.
Status:
Possibly Marketed Outside US
Source:
Japan:Cefminox Sodium
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cefminox is a broad-spectrum, bactericidal cephalosporin antibiotic. It is especially effective against Gram-negative and anaerobic bacteria. It is indicated in treatment of the following infections caused by sensitive bacteria: 1. Respiratory infections: Amygdalitis, circumtonsillar abscess, bronchitis, bronchiolitis, bronchiectasis (in fection), secondary infections of chronic respiratory diseases, pneumonia, and pulmonary suppuration; 2. Infection in urinary system: Nephropyelitis, cystitis; 3. Infections in abdominal cavity: Cholecystitis' angiocholitis'peritonitis; 4. Infections in pelvic cavity: Pelvic peritonitis, adnexitis, intrauterine infection, inflammation in pelvic dead space, and parametritis; 5. Septicaemia.
Status:
Possibly Marketed Outside US
Source:
ORAPENEM by Wyeth
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Tebipenem pivoxil is an oral carbapenem prodrug that was originated by Wyeth (now Pfizer). It was approved by Pharmaceuticals and Medical Devices Agency of Japan (PMDA) on Apr 22, 2009. It was developed and marketed as Orapenem® by Meiji Seika in Japan. Tebipenem pivoxil is a broad-spectrum orally-administered antibiotic, from the carbapenem subgroup of β-lactam antibiotics. Carbapenems are a class of beta-lactam antibiotics, which act by inhibiting the synthesis of the peptidoglycan layer of bacterial cell walls. It is used to treat otorhinolaryngological infection, otitis media and bacterial pneumonia. Orapenem® is available as granules for oral use, containing 100 mg Tebipenem pivoxil/g granules. According to the weight of children, 4 mg/kg, and twice a day after dinner.
Midecamycin diacetate (a derivative of Midecamycin) is reported as an ingredient of Miocamycin in Japan. Miocamycin is an orally administered 16-membered macrolide antimicrobial drug. It has a spectrum of in vitro activity similar to that of erythromycin, inhibiting a range of Gram-positive and Gram-negative organisms, atypical microbes and some anaerobes. Importantly, miocamycin demonstrates greater in vitro potency than erythromycin against several pathogens including Legionella pneumophila, Mycoplasma hominis, and Ureaplasma urealyticum. Equally noteworthy is its activity against erythromycin-resistant staphylococcal and streptococcal species expressing inducible-type resistance. Miocamycin possesses poor overall activity against Haemophilus influenzae and is inactive against Enterobacteriaceae. Penetration of miocamycin into body tissues and fluids is both rapid and extensive. The 3 major metabolites of miocamycin possess antimicrobial activity and may contribute to the therapeutic efficacy of the drug. Clinical data indicate that miocamycin is useful in the treatment of upper and lower respiratory tract infections in both adult and paediatric patients. Miocamycin is also effective in the treatment of urogenital tract infections caused by Chlamydia trachomatis or U. urealyticum. Midecamycin binds reversibly to 50S ribosomal subunit causing blockade of transpeptidation/translocation reactions, inhibition of protein synthesis and thus inhibition of cell growth. Midecamycin diacetate is also known as MIOCAMEN, Merced Box of 8 sachets (900mg), Mosil, Myoxam.
Micronomicin is a new aminoglycosidic antibiotic discovered and developed by Kyowa Hakko Kogyo Co., Ltd. It is produced by Micromonospora sagamiensis var. nonreducans. Investigation of micronomicin performed in 134 research facilities in Japan led to the following results. 1) Micronomicin showed a broad antibacterial spectrum against Gram positive and Gram negative bacteria. 2) In susceptibility tests of clinical isolates, micronomicin was almost similarly active to GM. 3) Bactericidal activity of micronomicin against Pseudomonas aeruginosa and E. coli was higher than those of TOB and DKB. 4) Micronomicin showed a synergistic antibacterial activity against Pseudomonas aeruginosa and E. coli with CBPC and SBPC. 5) The therapeutic activity of micronomicin in mice infected with Pseudomonas aeruginosa and Serratia sp. was in high correlation with in vitro antibacterial activity similarly to that of GM. Micronomicin (sold under the brand names Sagamicin and Luxomicina among others) is an aminoglycoside antibiotic, and like others in its class, binds to the ribosomes of non-resistant cells causing mistranscription of mRNA which fatally inhibits production of essential proteins. Micronomicin sulfate can inhibit bacterial protein synthesis, while destroy the bacterial cell wall. Micronomicin has an antibacterial activity against gram-negative and gram-positive bacteria such as Staphylococcus aureus, Staphylococcus epidermidis, Pseudomonas aeruginosa, Shara, Escherichia coli, etc. Streptococcus pneumoniae and Pneumococcus are sensitive to it, but its activity on anaerobic bacteria and some hemolytic streptococcus is weak.
Ribostamycin sulfate is an aminoglycoside-aminocyclitol antibiotic isolated from a streptomycete. It is an important broad-spectrum antibiotic with important use against human immunodeficiency virus and is considered a critically important antimicrobial by the World Health Organization. Aminoglycosides work by binding to the bacterial 30S ribosomal subunit (some work by binding to the 50S subunit), inhibiting the translocation of the peptidyl-tRNA from the A-site to the P-site and also causing misreading of mRNA, leaving the bacterium unable to synthesize proteins vital to its growth. Ribostamycin is usually used to treat sepsis, superficial skin infection, deep skin infection, lymphangitis/lymphadenitis, chronic pyoderma, osteomyelitis, pharyngitis/laryngitis, tonsillitis, acute bronchitis, pneumonia, pulmonary abscess, pyothorax, secondary infection in chronic respiratory lesions, cystitis, pyelonephritis, gonococcal infection, peritonitis, cholecystitis, dacryocystitis, keratitis (including corneal ulcer), otitis media, sinusitis and gnathitis. The most commonly reported adverse reactions include renal dysfunction, liver disorder and rash.

Showing 11 - 20 of 91 results