Aryl hydantoin Ro 13-3978, a broad-spectrum antischistosomal
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چکیده
منابع مشابه
Aryl hydantoin Ro 13-3978, a broad-spectrum antischistosomal.
OBJECTIVES Praziquantel is the only drug available for the treatment of schistosomiasis and the state of the exhausted drug discovery pipeline is alarming. We restarted investigations on the abandoned antischistosomal Ro 13-3978, an aryl hydantoin discovered in the early 1980s by Hoffmann La-Roche. METHODS Newly transformed schistosomula and adult Schistosoma mansoni were studied in the prese...
متن کاملRevisiting the SAR of the Antischistosomal Aryl Hydantoin (Ro 13-3978)
The aryl hydantoin 1 (Ro 13-3978) was identified in the early 1980s as a promising antischistosomal lead compound. However, this series of aryl hydantoins produced antiandrogenic side effects in the host, a not unexpected outcome given their close structural similarity to the antiandrogenic drug nilutamide. Building on the known SAR of this compound series, we now describe a number of analogs o...
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The pharmacokinetics of the new cephalosporin Ro-13-9904 were studied in six healthy male volunteers receiving a 500-mg dose as a bolus intravenously. Tissue penetration of the antibiotic was estimated by using a cantharides blister method. The data obtained fitted a two-compartment open model. The mean elimination half-life was about 8 h, which is considerably longer than that of other beta-la...
متن کاملRo 13-9904, a long-acting broad-spectrum cephalosporin: in vitro and in vivo studies.
Ro 13-9904, a new parenteral cephalosporin, was found to have high in vitro activity against Enterobacteriaceae and other gram-negative bacteria, including various isolates resistant to cefuroxime, cefamandole, cefoxitin, and cefazolin. It showed promising activity against Pseudomonas aeruginosa. Although inhibitory against Staphylococcus aureus at concentrations readily achievable in plasma, i...
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Ceftriaxone (Ro 13-9904) was compared with other newer beta-lactam antibiotics for activity in experimental infections of mice with Enterobacteriaceae, Haemophilus influenzae, Pseudomonas aeruginosa, and gram-positive bacteria. Overall, ceftriaxone was equal or superior to cefotaxime and cefoperazone against systemic infections. All three drugs were highly potent against most organisms but were...
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ژورنال
عنوان ژورنال: Journal of Antimicrobial Chemotherapy
سال: 2015
ISSN: 0305-7453,1460-2091
DOI: 10.1093/jac/dkv016