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

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Showing 571 - 580 of 2062 results

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)



2-Carboxy-2-Phenylethyl 1-(4-Chlorobenzoyl)-5-Methoxy-2-Methyl-1h-Indole-3-Acetate (Tropesin, VUFB-12018) is indometacin prodrug with potent anti-inflammatory efficacy and advantageous therapeutic properties. In experiments in vivo in rats, after oral administration of a Tropesin dose of 50 mg/kg, esterolysis was observed between 2-3, with a peak level of liberated indometacin between 10-13 h after ingestion. Tropesin was administered orally to rats and dogs in the daily therapeutic dose, triple the dose and ten times the dose for 3 months. After the highest dosage, in isolated cases, some dogs were found to have superficial erosions of the gastric mucosa and dystrophic lesions of renal tubules without biochemical correlations. Indometacin, administered in parallel doses, caused severe lesions of the gastrointestinal tract with melaena and subsequent anemia, as well as severe degenerative changes in renal tubules, in all dosage groups. From the toxicological aspect, Tropesin is substantially more acceptable than indomethacin. The anti-inflammatory and anti-arthritic activities of Tropesin in comparison with indomethacin, were studied in various models of both acute and chronic inflammatory reactions. Both compounds exhibited significant therapeutic activities without substantial quantitative differences.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

Tenuazonic acid is one of the major Alternaria mycotoxins commonly found as a natural contaminant in food. Tenuazonic acid contamination has been linked to esophageal cancer in human populations at risk of high exposure. Tenuazonic acid inhibits protein synthesis by suppression at the ribosome. Tenuazonic acid was shown to inhibit 12-O-tetradecanoyl phorbol-13-acetate (TPA) induced ornithine decarboxylase (ODC) activity in a mouse model, and in turn suppressed mouse skin tumor promotion. In addition, this compound has been shown to be a new type of Photosystem II inhibitor.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Isopimaric acid is a widely available tricyclic diterpenoid well represented in the resin of conifers of the genera Pinus, Larix, and Picea. It exhibits interesting biological and pharmaceutical properties such as antimicrobial, antiviral, antiallergenic, and anti‐inflammatory activities. It acts as a large conductance Ca2+activated K+ channel (BK channel) opener. BK channel openers have emerged as potentially useful agents in the therapy of various diseases associated with both the central nervous system and smooth muscle system.