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Restrict the search for
beta carotene
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Class (Stereo):
CHEMICAL (RACEMIC)
Pirazmonam is a potent anti-gram-negative monobactam that is differentiated from aztreonam by its high intrinsic activity against Ps. aeruginosa and good activity against Pseudomonas species. Pirazmonam has generally poor activity against gram-positive aerobic bacteria and anaerobic bacteria. Pirazmonam is a Trojan Horse molecule containing a b-lactam antibiotic that has been developed based on bacterial iron uptake systems. It features high structural similarity to aztreonam attached to a 3-hydroxy-4-pyridinone iron chelating group. Pirazmonam exhibited strong affinity to penicillin-binding protein 3 (PBP3) of Escherichia coli and moderate to negligible affinity to the other E. coli PBPs.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Quinacillin is semisynthetic penicillase-resistant penicillin patented by Boots Pure Drug Co. Ltd. For the treatment of bacterial infection. Quinacillin binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This interrupts bacterial cell wall synthesis and results in the weakening of the bacterial cell wall, eventually causing cell lysis. In clinical trials Staph. aureus was eradicated from all but two patients during treatment but recurred in 4 after withdrawal. The antibiotic was especially useful in the treatment of staphylococcal respiratory infections, as it has little effect on the normal bacterial flora of the chest.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Picumeterol (GR114297A) is a potent and highly selective beta2-adrenoceptor agonist with a longer duration of action than salbutamol, but shorter than salmeterol. Picumeterol is the (R)-isomer of the racemic entity GR63411B, and picumeterol has been shown to be about 40 times more potent than the (S)-isomer (GR114744A) in various in vitro pharmacological models of beta2-agonist activity. Picumeterol is of potential value in the treatment of asthma and related diseases in man following inhalation administration. In the clinical studies, the bronchodilator potencies of picumeterol and GR 63411B were similar. However, both drugs were short-acting, which is at odds with their activity in vitro. These compounds display dissociation between bronchodilator activity and protection against methacholine-induced bronchoconstriction.
Class (Stereo):
CHEMICAL (RACEMIC)
Trimeperidine (promedol) is the earliest and mostly studied opioid analgesic. Trimeperidine stimulates opioid receptors in the central nervous system. Compared with morphine, it has a weaker and shorter analgesic effect, less affects the respiratory, vomiting and vagal centers, does not cause smooth muscle spasm (except for the myometrium), and has a moderate antispasmodic and hypnotic effect. It is used to treat severe pain syndrome, acute left ventricular failure, pulmonary edema, cardiogenic shock, preparation for surgery, childbirth, high fever, post-transfusion complications, poisoning with atropine, barbiturates, barium, gasoline, boric acid, strong acids, carbon monoxide, turpentine, formalin, formalin. It has several side effects. Administration of this substance is associated with the development of life-threatening conditions accompanied by the suppression of respiration center. Analgesic trimeperidine (promedol) was included into the health care kits by various Ministries of the Russian Federation at different times.
Status:
Investigational
Source:
NCT00752011: Phase 1 Interventional Completed Cancer
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
3'-C-ethynylcytidine (Ethynylcytidine, TAS-106) is a synthetic cytidine nucleoside containing a covalently bound ethynyl group with potential antineoplastic and radiosensitizing activities. 3'-C-ethynylcytidine is metabolized in tumor cells to ethynylcytidine triphosphate (ECTP), which inhibits RNA synthesis by competitive inhibition of RNA polymerases I, II and III; subsequently, RNase L is activated, resulting in apoptosis. RNase L is a potent antiviral and antiproliferative endoribonuclease that cleaves singled stranded RNA, causes 28s rRNA fragmentation, and activates Janus Kinase (JAK), a mitochondrial-dependent apoptosis signaling molecule. Development of a cytosine derivative of 3'-ethynyl ribonucleoside, TAS-106, as an intravenously administered treatment for solid tumours was discontinued. A phase II trial in patients with head and neck cancer was terminated in the US.
Status:
Investigational
Source:
INN:loreclezole [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Loreclezole was found to be active in all animal models of seizures, whether a genetic model of reflex epilepsy was used or models where seizures were elicited by chemical or electrical stimulation. In addition, loreclezole was active against both TON and CLON seizures and increased the threshold for behavioral as well as EEG seizures. Loreclezole has a very rapid onset of action and a duration of the activity, which in certain tests last for more than 24 hr. Chronic administration for 5-7 days did not lead to tolerance to the anticonvulsant action of loreclezole. Loreclezole potentiates gamma-aminobutyric acid (GABA) type A receptor function, by interacting with a specific allosteric modulatory site on receptor beta-subunits. It also acts as a negative modulator at a novel regulatory site, enhancing GABAA receptor sensitization. Inhibits homomeric ρ1 GABAC receptors.
Status:
Investigational
Class (Stereo):
CHEMICAL (MIXED)
Status:
Investigational
Source:
USAN:CEFUROXIME PIVOXETIL [USAN]
Source URL:
Class (Stereo):
CHEMICAL (MIXED)
Cefuroxime Pivoxetil is an ester prodrug of cefuroxime, a semisynthetic, broad-spectrum, beta-lactamase-resistant, second-generation cephalosporin with antibacterial activity. Cefuroxime 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.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Ceftioxide is broad-spectrum , beta-lactam antibiotic patented by German pharmaceutical company Hoechst A.-G.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
TS-410 (Amelometasone), is a topical anti-inflammatory steroid. Amelometasone lotion - external steroid preparation - is marketed in Japan.
