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

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Showing 1 - 10 of 21 results

Tizoxanide, the primary active metabolite of the FDA approved drug nitazoxanide, an anti-infective that has been approved for the treatment of diarrhea caused by Giardia lamblia. Tizoxanide, an active metabolite of nitazoxanide in humans, is also an antiparasitic drug of the thiazolide class. It has broad-spectrum antiparasitic and broad-spectrum antiviral properties. Besides, it has being found that Tizoxanide exhibits appreciable antagonist activity for both mGluR1 and mGluR5 (IC50 = 1.8 uM and 1.2 uM, respectively).
Entacapone is a selective, reversible catechol-O-methyl transferase (COMT) inhibitor for the treatment of Parkinson's disease. It is a member of the class of nitrocatechols. When administered concomittantly with levodopa and a decarboxylase inhibitor (e.g., carbidopa), increased and more sustained plasma levodopa concentrations are reached as compared to the administration of levodopa and a decarboxylase inhibitor. The mechanism of action of entacapone is believed to be through its ability to inhibit COMT in peripheral tissues, altering the plasma pharmacokinetics of levodopa. When entacapone is given in conjunction with levodopa and an aromatic amino acid decarboxylase inhibitor, such as carbidopa, plasma levels of levodopa are greater and more sustained than after administration of levodopa and an aromatic amino acid decarboxylase inhibitor alone. It is believed that at a given frequency of levodopa administration, these more sustained plasma levels of levodopa result in more constant dopaminergic stimulation in the brain, leading to a greater reduction in the manifestations of parkinsonian syndrome. Entacapone is used as an adjunct to levodopa / carbidopa in the symptomatic treatment of patients with idiopathic Parkinson's Disease who experience the signs and symptoms of end-of-dose "wearing-off".
Status:
First approved in 1946
Source:
Streptomycin HCl by Philadelphia
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Streptomycin is a water-soluble aminoglycoside derived from Streptomyces griseus. Aminoglycosides work by binding to the bacterial 30S ribosomal subunit, causing misreading of t-RNA, leaving the bacterium unable to synthesize proteins vital to its growth. Aminoglycosides are useful primarily in infections involving aerobic, Gram-negative bacteria, such as Pseudomonas, Acinetobacter, and Enterobacter. In addition, some mycobacteria, including the bacteria that cause tuberculosis, are susceptible to aminoglycosides. Infections caused by Gram-positive bacteria can also be treated with aminoglycosides, but other types of antibiotics are more potent and less damaging to the host. In the past the aminoglycosides have been used in conjunction with penicillin-related antibiotics in streptococcal infections for their synergistic effects, particularly in endocarditis. Aminoglycosides are mostly ineffective against anaerobic bacteria, fungi and viruses. Aminoglycosides like Streptomycin "irreversibly" bind to specific 30S-subunit proteins and 16S rRNA. Specifically Streptomycin 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. Streptomycin is indicated for the treatment of tuberculosis. May also be used in combination with other drugs to treat tularemia (Francisella tularensis), plague (Yersia pestis), severe M. avium complex, brucellosis, and enterococcal endocarditis (e.g. E. faecalis, E. faecium).
Status:
Investigational
Source:
INN:thiazosulfone [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Thiazosulfone (also known as Promizole) is a phenylsulfonylthiazole derivative patented by Parke, Davis & Co. as the anti-tuberculosis agent. In preclinical models, Thiazosulfone exerts a definitely favorable influence on the course of experimental tuberculosis previously established in the highly susceptible guinea pig. In clinical trials Thiazosulfone and Streptomycin combined therapy exerts favor influences on tuberculous meningitis. Thiazosulfone seems to have an inhibitory action on hematogenous tuberculosis. Its toxicity is very low and it can, therefore, be administered for a prolonged period.
Status:
Investigational
Source:
INN:thiambutosine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Thiambutosine is a carbanilide derivative patented by Imperial Chemical Industries Ltd. as the antituberculous agent. In vitro, the resistance of Mycobacterium tuberculosis H37Rv to Thiambutosine develops more slowly than resistance to streptomycin, p-aminosalicylic acid, or isoniazid. A sub-inhibiting concentration of Thiambutosine with either streptomycin or isoniazid considerably retards the emergence of strains resistant to these two agents.
Status:
Investigational
Source:
INN:hetaflur [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Cetylamine is an aliphatic primary amine that possesses surface-active properties and widely used in water treatment. Cetylamine shows moderate anti-tuberculosis activity. Cetylamine also may be used as a source of fluoride in the prevention of dental caries.
Picromycin was studied by Brokmann and Hekel in 1951 and was the first antibiotic macrolide to be isolated. Picromycin is not a clinically useful antibiotic, it can be used as a raw material to synthesize antibiotic ketolide compounds such as ertythromycins and new epothilones. Picromycin is an antibiotic active mainly against gram-positive bacteria.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Nidulin is a depsidone produced by several fungal species with potent and selective antibacterial activity. Nidulin revealed a potent aromatase inhibitory activity.
Cloxyquin has being shown to be a novel activator of the two-pore domain potassium channel TRESK, which is linked to causing migraines and controls the sensitivity of pain nerves in the brain.