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

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Showing 331 - 340 of 470 results

Status:
Investigational
Source:
INN:soterenol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Soterenol [(+)-1-(3-methanesulphonamido, 4-hydroxyphenyl)-2-isopropylaminoethanol, MJ 1992] is a directly acting sympathomimetic amine which has been shown to display Beta2-adrenoceptor selectivity. Soterenol, a methanesulfonamido-phenethanolamine related structurally to isoproterenol, was a highly effective bronchodilator agent in several animal species by various routes of administration. The bronchodilator potency of soterenol was equivalent to, or greater than, that of isoproterenol. Soterenol also had potent stimulant action on the alpha-receptor of the smooth muscle.
Status:
Investigational
Source:
INN:sancycline
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

There is a little information around sancycline. It is known, that it was synthesized by Conover and co-workers in 1962 and it was antibacterial compound. It was proposed that sancycline binds to the 30S of bacterial ribosomal subunit and inhibiting protein translation by blocking entry of aminoacyl-tRNA into the ribosome A site.
Status:
Investigational
Source:
NCT00028782: Not Applicable Interventional Terminated Advanced Malignant Mesothelioma
(2001)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Etanidazole (also known as Radinyl) is a 2-nitroimidazole with radiosensitizing properties. Etanidazole exerts its therapeutic action by depleting glutathione and inhibiting glutathione S-transferase, thus enhancing the anticancer effects of radiation therapy. Etanidazole was tested in Phase III clinical trials in patients with advanced head and neck cancer, however, its development was stopped. A fluorinated etanidazole (EF5) may also be useful as an imaging agent for identification of hypoxic, drug-resistant regions of primary tumors and metastases.
Status:
Investigational
Source:
INN:tigemonam
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Tigemonam is a dialkylazetidinone derivative patented by E. R. Squibb and Sons, Inc. as a beta-lactam agent useful for the treatment of bacterial infections. Of the orally active beta-lactams, tigemonam is one of the most potent, with a spectrum of activity similar to that of aztreonam and highly resistant to hydrolysis by the beta-lactamase enzymes. Tigemonam inhibits 90% of Escherichia coli, Klebsiella spp., Proteus spp., Salmonella spp., Haemophilus influenzae and Branhamella catarrhalis tested. In localized infections, tigemonam also demonstrated excellent in vivo activity. In acute pyelonephritis in mice caused by Escherichia coli or Proteus sp., tigemonam was very effective. In a rat lung model with Klebsiella pneumoniae, tigemonam was active with a median effective dose of 46 mg/kg compared with 160 mg/kg for cefaclor and over 200 mg/kg for amoxicillin.
Status:
Investigational
Source:
NCT02253342: Phase 1 Interventional Completed Intrapulmonary Pharmacokinetics of WCK 2349
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Levonadifloxacin is the S-(-) isomer of the benzoquinolizine fluoroquinolone nadifloxacin and is two- to four-fold more active than the racemic mixture. Levonadifloxacin is a potent antibacterial agent against Gram-positive bacteria especially against methicillin resistance Staphylococcus aureus. It also possesses potent bactericidal activity against other resistant variants like quinolone-resistant Staphylococcus aureus, vancomycin and glycopeptide intermediate Staphylococcus aureus and vancomycin resistant Staphylococcus aureus. Intravenous dosage form developed to treat complicated skin and skin structure infections and has recently completed Phase III studies in India and Phase I studies in USA.
Status:
Investigational
Source:
NCT02253342: Phase 1 Interventional Completed Intrapulmonary Pharmacokinetics of WCK 2349
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Levonadifloxacin is the S-(-) isomer of the benzoquinolizine fluoroquinolone nadifloxacin and is two- to four-fold more active than the racemic mixture. Levonadifloxacin is a potent antibacterial agent against Gram-positive bacteria especially against methicillin resistance Staphylococcus aureus. It also possesses potent bactericidal activity against other resistant variants like quinolone-resistant Staphylococcus aureus, vancomycin and glycopeptide intermediate Staphylococcus aureus and vancomycin resistant Staphylococcus aureus. Intravenous dosage form developed to treat complicated skin and skin structure infections and has recently completed Phase III studies in India and Phase I studies in USA.
Status:
Investigational
Source:
NCT02253342: Phase 1 Interventional Completed Intrapulmonary Pharmacokinetics of WCK 2349
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Levonadifloxacin is the S-(-) isomer of the benzoquinolizine fluoroquinolone nadifloxacin and is two- to four-fold more active than the racemic mixture. Levonadifloxacin is a potent antibacterial agent against Gram-positive bacteria especially against methicillin resistance Staphylococcus aureus. It also possesses potent bactericidal activity against other resistant variants like quinolone-resistant Staphylococcus aureus, vancomycin and glycopeptide intermediate Staphylococcus aureus and vancomycin resistant Staphylococcus aureus. Intravenous dosage form developed to treat complicated skin and skin structure infections and has recently completed Phase III studies in India and Phase I studies in USA.
Status:
Investigational
Source:
INN:clinafloxacin
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Clinafloxacin is a broad-spectrum fluoroquinolone antibiotic that was originally developed and subsequently abandoned in the late 1990s as a human health antibiotic for respiratory diseases. Clinafloxacin displays broad-spectrum antibacterial activity against Gram-positive, Gram-negative, and anaerobic pathogens by inhibiting the bacterial regulatory enzyme DNA gyrase (IC50 = 0.92 ug/ml) as well as topoisomerase IV (IC50 = 1.62 ug/ml).
Status:
Investigational
Source:
INN:lamifiban
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


LAMIFIBAN is a potent and selective nonpeptide glycoprotein IIb/IIIa antagonist. It inhibits platelet aggregation and thrombus formation by preventing the binding of fibrinogen to platelets. It was in clinical development as an injectable antithrombotic agent for treating and preventing acute coronary syndromes but showed no significant effects on clinical outcomes.
Status:
Investigational
Source:
INN:puromycin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Puromycin dihydrochloride belongs to the aminonucleoside family of antibiotics and is isolated from Streptomyces alboniger. Since the partial structure of this antibiotic showed it to be a purine derivative, puromycin was assigned as its generic name. Puromycin is a broad spectrum antibiotic and antibacterial agent. It is active against Gram-positive microorganisms, less active against acid-fast bacilli, and weakly active against Gram-negative microorganisms. It acts very quickly and can kill 99% of the cells within 2 days. It also exhibits antitumor activity in studies on brain tumor cells. Puromycin is a protein synthesis inhibitor that causes premature chain termination by acting as an analog of the 3’-terminal end of aminoacyl-tRNA. It has been used to study transcriptional regulatory mechanisms that control the sequential and coordinate expression of genes during cell differentiation.

Showing 331 - 340 of 470 results