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

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Showing 341 - 350 of 657 results

Cefcapene is a semisynthetic third-generation cephalosporin with antibacterial activity. Cefcapene 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.
Etafenone is an antiarrhythmic and coronary vasodilator drug. Etafenone exerts negative inotropic action on myocardium. It is able to block calcium channels. As a coronary vasodilator which produces a decrease in the heart rate and myocardial oxygen consumption, etafenone has been used in the therapy of ischemic heart disease.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Ancarolol is a beta-adrenoceptor antagonist which can be used therapeutically as an antihypertensive.
Status:
Possibly Marketed Outside US
Source:
Ceftezole sodium for injection by Fujisawa Pharmaceutical
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Ceftezole sodium is a cephalosporin antibiotic. Ceftezole was found to be a broad-spectrum antibiotic, active in vitro against many species of gram-positive and gram-negative bacteria except Pseudomonas aeruginosa, Serratia marcescens and Proteus vulgaris. Ceftezole sodium is used as an injectable or through an intravenous mode of delivery. The bactericidal activity of ceftezole results from the inhibition of cell wall synthesis via affinity for penicillin-binding proteins (PBPs). The PBPs are transpeptidases which are vital in peptidoglycan biosynthesis. Therefore, their inhibition prevents this vital cell wall component from being properly synthesized. Ceftezole has been shown to exhibit potent alpha-glucosidase inhibitory activity. In in vitro alpha-glucosidase assays, ceftezole was shown to be a reversible, non-competitive inhibitor of yeast alpha-glucosidase with a Ki value of 5.78 x 10(-7) M when the enzyme mixture was pretreated with ceftezole. Ceftezole is used for the treatment of susceptible bacterial infections including septicemia, respiratory, biliary or GU tract, skin and skin structure, endocarditis. Surgical prophylaxis.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)


Carazolol is a beta1/beta2 adrenoreceptor blocking agent. Activity and safety of the drug were evaluated in clinical trials that were conducted in healthy subjects and in patients suffering from either chronic bronchitis or asthma. The drug, however, was not developed for human use. Instead, carazolol is used in to reduce stress in animals during transportation. In veterinary medicine, carazolol is given by intramuscular injection to pigs is indicated in stress-inducing situations. In cattle, carazolol is intended to be used for the prevention of shipment stress caused by transportation and formation of new herds.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Apalcillin is a naphthydridine derivative of ampicillin. Apalcillin has a broad spectrum of antibacterial activity that is very similar to that of piperacillin, except that apalcillin is significantly more active against Pseudomonas aeruginosa and Acinetobacter spp. Against Acinetobacter spp., apalcillin is uniquely active, compared to the other penicillins and comparison drugs. Strains producing high amounts of β-lactamases do become resistant to apalcillin. PAH (p-aminohippurate) clearance was significantly decreased during apalcillin infusion. Apalcillin appeared to compete with PAH for proximal tubular secretion but induced no further renal dysfunction.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)


Alfurolol is a beta-adrenergic blocker. It is non-selective blocking drug with both intrinsic sympathomimetic activity and weak membrane stabilizing activity. There is also evidence that, unlike other beta-blocking drugs, only extremely small amounts of alfurolol cross the blood-brain barrier: because of this property, it has very little effect on the CNS. Alfurolol consistently produced a reduction in exercise heart rate at all times during the seven-hour period of observation, and the reductions were significantly different from the corresponding values after placebo treatment. Alfurolol is active both on heart rate and systolic pressure.
Status:
Possibly Marketed Outside US
Source:
Japan:Cefpimizole Sodium
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Cefpimizole is an antibiotic of broad spectrum developed in Japan for the treatment of such conditions as uncomplicated gonorrhea and gynecologic infections. The drug was tested in clinical trials, however, its development was terminated.
Status:
Possibly Marketed Outside US
Source:
Japan:Cefmatilen Hydrochloride Hydrate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cefmatilen (codenamed S-1090) is an orally-active cephalosporin antibiotic, that shows high activity against a variety of Gram-positive and Gram-negative bacteria, including Streptococcus pyogenes and Neisseria gonorrhoeae.
Status:
Possibly Marketed Outside US
Source:
Carbenin by Daiichi Sankyo
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Panipenem is a parenteral carbapenem antibacterial agent with a broad spectrum of in vitro activity covering a wide range of Gram-negative and Gram-positive aerobic and anaerobic bacteria, including Streptococcus pneumoniae and species producing β-lactamases. Panipenem is coadministered with betamipron (Carbenin, Daiichi Sankyo Company) to inhibit panipenem uptake into the renal tubule and prevent nephrotoxicity. In large, randomised clinical trials, panipenem/betamipron demonstrated good clinical and bacteriological efficacy (similar to that of imipenem/cilastatin) in adults with respiratory tract or urinary tract infections.

Showing 341 - 350 of 657 results