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

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Showing 8221 - 8230 of 141793 results

Status:
Investigational
Source:
INN:tomopenem [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Tomopenem (formerly CS-023) is a 1β-methylcarbapenem with improved activity against diverse hospital pathogens, including Pseudomonas aeruginosa and methicillin-resistant Staphylococcus aureus (MRSA), and has a half-life about twice longer than the half-lives of other carbapenems such as imipenem (IPM) and meropenem (MEM). In vitro activity of tomopenem is comparable to that of IPM against most isolates of Gram-positive pathogens and similar to that of MEM against Gram-negative pathogens. Furthermore, tomopenem displayed improved activity against not only P. aeruginosa but also MRSA compared to IPM and MEM. In addition to the improved activity, tomopenem showed a half-life about twice longer than that of IPM or MEM in humans. The affinity of tomopenem for penicillin-binding protein (PBP) 2a might be higher than that of IPM. Tomopenem had been in phase II clinical trial for the treatment of Gram-positive and Gram-negative bacterial infection. However, this development was discontinued.
Status:
Investigational
Source:
INN:thymocartin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Thymocartin (also known as T4 and RGH-0206) is a protected synthetic tetrapeptide patented by Hungarian multinational pharmaceutical and biotechnology company Gedeon Richter Plc. (Richter, Gedeon, Vegyeszeti Gyar Rt) as an immunomodulating agent. In preclinical models, Thymocartin shows to exert similar immunomodulatory activities to thymopoietin affecting both humoral and cellular responses. In skin graft mouse model Thymocartin increases the number of splenic T cells and restored the rejection capacity of thymectomized C57Bl mice. In chronic 28-days i.v. toxicity studies in dogs no adverse reaction has been found. The low toxicity of Thymocartin is probably attributable to their short half-life as the half-life of the Thymocartin is less than 3 min in humans.
Status:
Investigational
Source:
INN:tioxacin
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Tioxacin is a bactericide agent. Tioxacin gives a soluble complex with aliphatic amines and had the highest activities against G(+) and G (-) bacteria, including Escherichia coli resistant to nalidixic acid and Pseudomonas aeruginosa from 98 acids of this type. Absorption studies in dogs suggested that the amine complex may have a great utility as a rapid dissolving form of tioxacin in oral administration.
Status:
Investigational
Source:
INN:tioctilate [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Tioctilate is a benzoic acid derivative patented by Chevron Research Co. as an acaricide and ovicide. Tioctilate is rapidly degraded by a soil extract under aerobic conditions.
Status:
Investigational
Source:
INN:tipindole [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Tipindole is serotonin antagonist. It is a monamine oxidase inhibitor. Diarrhea that arises in mice given serotonin intravenously is not suppressed by tipindole. Tipindole exerts no effect on the serotonin-induced contraction and relaxation of the bladder detrusor. Tipindole depresses reflexes from pericardial receptors considerably more than reflexes from carotid sinus receptors. Tipindole blocks chemoreceptors but has no effect on mechanoreceptors – it did not modify impulses produced by mechanoreceptors.
Status:
Investigational
Source:
INN:tiqueside [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Tiqueside is the synthetic spirostane-based steroid glycoside. It precipitates cholesterol from micellar solution in vitro and reduces plasma cholesterol absorption in rats through a mechanism that is currently thought to be independent of either association of the saponin with the intestinal mucosal surface or absorption of the saponin molecule. As a consequence of this inhibition, tiqueside has been shown to reduce plasma cholesterol concentrations in cynomolgus monkeys. Inhibition of cholesterol absorption by tiqueside produces profound effects on cholesterol metabolism without affecting bile acid metabolism, and these changes lead to reductions primarily in plasma non-HDL cholesterol concentrations. Tiqueside produced a dose-dependent reduction in plasma LDL cholesterol levels in the hypercholesterolemic patients. In the mechanistic study, it decreased fractional cholesterol absorption rates and increased fecal neutral sterol excretion rates, changes associated with trends toward lower LDL cholesterol levels. Other lipoprotein levels were unaffected, as were fecal fat and bile acid excretion and fat-soluble vitamin absorption. Thus tiquesidedose-dependently inhibits cholesterol absorption in humans, resulting in a reduction in serum LDL cholesterol levels.
Status:
Investigational
Source:
INN:tiviciclovir [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Tiviciclovir (A188) is a nucleoside analog used in the synthesis of antiviral drugs. This acyclic guanosine analog has a potential for the treatment of hepatitis B virus. However, as with penciclovir and the related compounds acyclovir and ganciclovir, the intestinal absorption of Tiviciclovir is limited. One approach to overcome this is through synthesis of the 6-deoxy prodrug version of AM188, i.e. AM365, which has improved intestinal absorption. Following absorption, the 6-deoxyguanosine analog AM365 is converted to the corresponding anti-virally active guanosine analog, AM188, probably by the liver molybdenum hydroxylases, aldehyde oxidase and xanthine oxidase. Renal tubular secretion of AM188 involves organic anion and cation transport systems.
Status:
Investigational
Source:
INN:tobuterol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Tobuterol is a bronchodilator agent. It is a beta2-adrenergic ligand.
Status:
Investigational
Source:
INN:tizolemide [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Tizolemide is a sulphonamide diuretic. The effect on transepithelial Na transport of tizolemide was investigated in isolated frog skin (Rana temporaria). It was found that tizolemide (2-5 mM, serosal side) decreased transepithelial Na transport (measured as short circuit current and as net sodium flux) within 60 min to 25-40% of the control level resulting from reduction of the unidirectional sodium influx. Tizolemide has alkaline properties and is cleared by a tubular transport system which differs from the PAH-excreting system which transports thiazide diuretics. Tizolemide was almost completely absorbed from the gastrointestinal tract. The drug was mainly eliminated via tubular secretion. Renal clearance of the drug was much lower in patients with compensated cardiac failure than in healthy subjects because of low renal plasma flow. As a consequence, plasma half-life was prolonged considerably in some patients. It was concluded that drugs with mainly tubular renal elimination may have a reduced elimination rate in patients with cardiac diseases despite normal glomerular filtration rate.
Status:
Investigational
Source:
NCT00691132: Phase 2 Interventional Completed Lung Cancer
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Phenethyl isothiocyanate (PEITC) presents in cruciferous vegetables which have been shown to decrease the risk of various types of malignancies. PEITC targets multiple proteins to suppress various cancer-promoting mechanisms such as cell proliferation, progression and metastasis. PEITC induces apoptosis in human colon cancer HT-29 cells, prostate cancer cells, and osteogenic sarcoma U-2 OS cells. Unique to prostate cancer is that PEITC downregulates the transcriptional factor Sp1, a regulator of AR expression. PEITC suppresses 4-(methylnitrosamino)-1-(3-pyridyl)-1-butoneinduced pulmonary neoplasia in A/J mouse lung, exhibits cancer chemopreventive activity in rat and reduces azoxymethane-induced colonic aberrant crypt foci formation. PEITC appears to be a promising agent for cancer therapy and is already under clinical trials for leukemia and lung cancer.

Showing 8221 - 8230 of 141793 results