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Restrict the search for
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Class (Stereo):
CHEMICAL (ABSOLUTE)
Cefrotil is an antibiotic drug patented by pharmaceutical company Farbwerke Hoechst A.-G.
And used as pharmaceutical intermediates
Class (Stereo):
CHEMICAL (ABSOLUTE)
Cefaloram is aminocephalosporanic acid derivative with potent antibacterial activity. Cefaloram 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
Status:
Investigational
Source:
INN:difencloxazine [INN]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Difencloxazine is a tranquilizing agent.
Status:
Investigational
Source:
NCT02265289: Phase 1 Interventional Completed Healthy
(1999)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Lefradafiban, an orally active prodrug of fradafiban, is a novel glycoprotein (IIb/IIIa) inhibitor for the treatment of unstable angina. The pharmacokinetic and pharmacodynamic properties of lefradafiban were assessed in 130 healthy male volunteers who received a single dose of 10, 50, 75, 100, or 150 mg or multiple doses of 25, 50, 60, 75, 90, or 100 mg three times daily for one week. After both single and multiple doses, receptor occupancy and plasma lefradafiban levels correlated with platelet aggregation. Lefradafiban had been in phase II clinical trials by Boehringer Ingelheim for the treatment of thrombosis. However, it has been terminated.
Status:
Investigational
Source:
NCT01128335: Phase 2 Interventional Completed Liver Transplantation
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Sotrastaurin, an orally-active, first-in-class immunomodulator, is under development by Novartis for the treatment of uveal melanoma and diffuse-large B-cell lymphoma. Sotrastaurin is a low molecular mass synthetic compound
that potently inhibits the PKC α, β and the θ isoforms
resulting in selective NF-κB inactivation. Sotrastaurin is a potent and selective pan-PKC inhibitor, mostly for PKCθ with Ki of 0.22 nM in a cell-free assay. Inhibition of PKC beta in B-cells results in prevention of NF-kB-mediated signaling and down regulation of NF-kB target genes. This may eventually lead to an induction of G1 cell cycle arrest and tumor cell apoptosis in susceptible tumor cells. This agent may act synergistically with other chemotherapeutic agents. PKC, a family of serine/threonine protein kinases overexpressed in certain types of cancer cells, is involved in cell differentiation, mitogenesis, inflammation, and the activation and survival of lymphocytes. Sotrastaurin is currently in phase II trials by Novartis for the treatment of large B-cell lymphoma and uveal melanoma. Sotrastaurin was in Phase II of clinical development for the prevention of acute rejection after solid organ transplantation and psoriasis, but this reseach had being discontinued.
Class (Stereo):
CHEMICAL (RACEMIC)
Procinolol is phenoxypropanol derivative patented by Societe Industrielle pour la Fabrication des Antibiotiques for treating angina and cardiac rhythm disorders
Class (Stereo):
CHEMICAL (RACEMIC)
Pargolol (also Kö 1400) is a beta-adrenergic receptor blocking agent that was developed as an antiarrhythmic agent. However, information about the further development of this drug is not available.
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 (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.
