Biomedical subjects

N Jiraskova

Publications and source records attributed to N Jiraskova.

4 recordsLinked to original sources

PubMed2001

MEN-10700 menarini.

Menarini is investigating the penem beta-lactam antibiotic, MEN-10700, for the potential control of bacterial infections. MEN-10700 compares favorably with other oral beta-lactams against Haemophilus influenzae strains as well as other respiratory pathogens [341073]. The compound has also showed activity against multiple drug-resistant Gram-negative pathogens [341074]. MEN-10700 has a broad spectrum of activity against Gram-positive and Gram-negative bacteria and demonstrates a potency greater than that of imipenem [174404].

Anti-Bacterial Agents↗

PubMed2001

RWJ-333441 Microcide/RW Johnson.

Microcide and RW Johnson Pharmaceutical Research Institute are investigating a novel cephalosporin prodrug RWJ-333442 for the potential treatment of bacterial infections. RWJ-333442 is the prodrug of RWJ-333441; it has an improved solubility profile and studies are in progress in human serum, rats and rhesus macaques [382578], [382862], [383594].

Anti-Bacterial Agents↗

PubMed2001

THF carbapenems. Wyeth Ayerst.

CL-191121 is one of three new tetrahydrofuranyl (THF) carbapenems, which possess stability to renal dihydropeptidase and beta-lactamases [162484], [387167], [418244] and have minimal binding to penicillin-binding proteins (PBPs) [163188]. Of the series of THF carbapenems, CL-191121 had the best activity against gram-positive organisms, particularly against Enterococcus faecalis. It demonstrated moderate oral activity against an Escherichia coli infection in mice and was 20-fold more efficacious than imipenem [253186]. As the effective oral dose (ED50) was 11- to 14-fold higher than the effective subcutaneous dose, a series of bis-double ester prodrugs (of the aminomethyl-THF 1beta-methyl-carbapenems) was prepared, which showed substantially improved oral bioavailability in the mouse model (EU50 = 0.42 microg/ml following a single oral dose obtained for the most potent compound) [258726]. OCA-983 is a prodrug derivative of CL-191121 sharing potent inhibitory activity against class A and class C beta-lactamases [324244], although development of this compound is no longer being pursued.

Anti-Bacterial Agents↗

PubMed2000

Olamufloxacin. Hokuriku Seiyaku.

Hokuriku is developing olamufloxacin, a quinolone antibiotic that inhibits DNA gyrase, for the potential treatment of various types of bacterial infection. It has reached late phase II clinical trials. An intravenous formulation is also under investigation [277817].

Animals↗