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

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Showing 31 - 40 of 234 results

Status:
US Previously Marketed
Source:
Siseptin by Schering
(1980)
Source URL:
First approved in 1980
Source:
Siseptin by Schering
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Sisomicin is a new broad-spectrum aminoglycoside most closely related structurally to gentamicin C1a. In vitro and in experimental infections, sisomicin has been found to be more potent than or nearly as potent as the most active of the other available aminoglycosides. Although susceptible to many (but not all) aminoglycoside-inactivating enzymes, sisomicin is active against many microorganisms that are resistant to other aminoglycosides by nonenzymatic mechanisms. Sisomicin has been shown to interact synergistically with various beta-lactam antibiotics against enterococci, staphylocicci, Enterobacteriaceae, and nonfermentative gram-negative bacilli. The pharmacokinetics and toxicity of sisomicin in humans appear to be similar to those of gentamicin, despite earlier reports of greater acute toxicity in animals. Sisomicin binds to 30s and 50s ribosomal subunits of susceptible bacteria disrupting protein synthesis, thus rendering the bacterial cell membrane defective.
Cyclacillin is a cyclohexylamido analog of penicillanic acid. It is used for the treatment of bacterial infections caused by susceptible organisms. Cyclacillin is more resistant to beta-lactamase hydrolysis than ampicillin, is much better absorbed when given by mouth and, as a result, the levels reached in the blood and in the urine are considerably higher than those obtained with the same dose of ampicillin. The bactericidal activity of cyclacillin results from the inhibition of cell wall synthesis via affinity for penicillin-binding proteins (PBPs). Cyclacillin has been replaced by newer penicillin treatments.
Status:
US Previously Marketed
Source:
Utibid by Warner/Chilcott
(1975)
Source URL:
First approved in 1975
Source:
Utibid by Warner/Chilcott
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Oxolinic acid is a synthetic quinolone antibiotic related to nalidixic acid. It is authorized in veterinary medicine for use in finfish, calves, pigs, and poultry. It acts by inhibiting bacterial type II topoisomerase activity. Oxolinic acid has been used in human medicine in several countries in the past. Its use in human medicine has largely been replaced by the fluoroquinolone antibiotics.
Status:
US Previously Marketed
First approved in 1974

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cephapirin is a first-generation cephalosporin. Cephapirin has been indicated for the treatment of infections when caused by susceptible strains in respiratory, genitourinary, gastrointestinal, skin and soft tissue, bone and joint infections, septicemia; treatment of susceptible gram-positive bacilli and cocci (never enterococcus); some gram-negative bacilli including E. coli, Proteus, and Klebsiella may be susceptible. Cephapirin is used in veterinary as an intra-uterine antibiotic infusion for the treatment of subacute and chronic endometritis in cows and repeat breeders.
Status:
US Previously Marketed
First approved in 1970

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cephaloglycin, first oral cephalosporin, was introduced in 1965, but is no longer in common use. It is an orally absorbed derivative of cephalosporin C. Cephaloglycin binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.
Status:
US Previously Marketed
Source:
COLGATE TOTAL by COLGATE PALMOLIVE
(1997)
Source URL:
First approved in 1969
Source:
P-300 Antibacterial by Colgate-Palmolive
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Triclosan was used as a hospital scrub in the 1970s. Since then, it has expanded commercially and is now prevalent in soaps (0.10-1.00%), shampoos, deodorants, toothpastes, mouth washes, cleaning supplies and pesticides. It is part of consumer products, including kitchen utensils, toys, bedding, socks and trash bags. In healthcare, triclosan is used in surgical scrubs and hand washes. Use in surgical units is effective with a minimum contact time of approximately two minutes. More recently, showering with 2% triclosan has become a recommended regimen in surgical units for the decolonization of patients whose skin carries methicillin-resistant Staphylococcus aureus (MRSA). Triclosan is also used in the coatings for some surgical sutures. Triclosan has been employed as a selective agent in molecular cloning. At high concentrations, triclosan acts as a biocide with multiple cytoplasmic and membrane targets. However, at the lower concentrations seen in commercial products, triclosan appears bacteriostatic, and it targets bacteria primarily by inhibiting fatty acid synthesis. Triclosan binds to bacterial enoyl-acyl carrier protein reductase (ENR) enzyme, which is encoded by the gene FabI. This binding increases the enzyme's affinity for nicotinamide adenine dinucleotide (NAD+). This results in the formation of a stable, ternary complex of ENR-NAD+-triclosan, which is unable to participate in fatty acid synthesis. Fatty acids are necessary for building and reproducing cell membranes. Humans do not have an ENR enzyme and thus are not affected.
Status:
US Previously Marketed
First approved in 1964

Class (Stereo):
CHEMICAL (ACHIRAL)


Lapyrium, or lapirium, as the chloride salt lapirium chloride (INN) or lapyrium chloride (USAN), is a cationic surfactant that is used in cosmetic personal care products as a biocide and antistatic agent. A 50% solution of Lapyrium Chloride produced slight to moderate erythema. Lapyrium is also used in waste-water treatment and corrosion inhibition formulations.
Status:
US Previously Marketed
First approved in 1963

Class (Stereo):
CHEMICAL (ACHIRAL)



Sulfaphenazole is an oral antibiotic, which was used for the treatment of bacterial infections under the name Sulfabid. The drug was found to block folate synthesis in bacterias by inhibiting the enzyme dihydropteroate synthase. Sulfaphenazole is also known to inhibit CYP2C9 with high potency and specificity. Sulfabid is no longer marketed in the USA.
Status:
US Previously Marketed
First approved in 1960
Source:
Staphcillin by Bristol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Methicillin sodium anhydrous is a sodium salt of methicillin (methicillin). Methicillin is an antibiotic formerly used in the treatment of bacterial infections caused by organisms of the genus Staphylococcus. Methicillin is a semisynthetic derivative of penicillin. It was first produced in the late 1950s and was developed as a type of antibiotic called penicillinase-resistant penicillin—it contained a modification to the original penicillin structure that made it resistant to a bacterial enzyme called penicillinase (beta-lactamase). Compared to other penicillins that face antimicrobial resistance due to β-lactamase, it is less active, can be administered only parenterally, and has a higher frequency of interstitial nephritis, an otherwise-rare adverse effect of penicillins. However, the selection of meticillin depended on the outcome of susceptibility testing of the sampled infection, and since it is no longer produced, it is also not routinely tested for anymore.
Status:
US Previously Marketed
Source:
Septiderm by Fougera
(1960)
Source URL:
First approved in 1960
Source:
Septiderm by Fougera
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Chloroxylenol is used as a preservative in cooling fluids, cosmetics, topical medications, urinary antiseptics and metal working fluids. Products containing Chloroxylenol are used for cleaning and disinfecting wounds, abrasions and abscesses, for minor cuts and scratches, insect bites, burns, inflammation of the skin. It is also found in hair conditioners, toilet cleaners, deodorants, soaps and paste. New use cases continue to be identified. Chloroxylenol has been shown to be effective at reducing the number of pathogenic bacteria in clinical environments. Chloroxylenol has been reviewed and is permitted for use within the European Union (EU) in cosmetic products and is also permitted for use in a number of topical pharmaceutical products as licensed by the UK Medicines and Health Regulatory Agency. Chloroxylenol could cause mild skin irritation in some individuals, or cause an allergic reaction in others. Developed in Europe in the 1920s and used in the United States since the 1950s, Chloroxylenol is one of the most mature antimicrobial agents