Anti-bacterial drugs have “selective toxicity”, that is they interact with a target present on the bacterial cell, the prokaryote, that is not present in the mammalian host, the eukaryote. For the ß-lactam drugs, this target is the cell wall. Mammalian cells lack cell walls, which for the bacteria are a critically important barrier protecting the organism from not only the vagaries of osmotic s...

OBJECTIVE To compare the effectiveness and toxicity of ciprofloxacin vs an aminoglycoside, both in combination with a beta-lactam, for the treatment of febrile neutropenia in the inpatient setting. METHODS For this meta-analysis of randomized controlled trials (RCTs) that compared the ciprofloxacin/beta-lactam combination vs an aminoglycoside/beta-lactam combination for the treatment of febri...

OBJECTIVE To compare the effectiveness of beta lactam monotherapy versus beta lactam-aminoglycoside combination therapy in the treatment of patients with fever and neutropenia. DATA SOURCES Medline, Embase, Lilacs, the Cochrane Library, and conference proceedings to 2002. References of included studies and contact with authors. No restrictions on language, year of publication, or publication ...

An increase in the number of tuberculosis cases caused by multiple-drug-resistant strains of Mycobacterium tuberculosis has stimulated search for new antituberculous agents. Beta-lactam antibiotics, traditionally regarded as ineffective against tuberculosis, merit consideration. Four major penicillin-binding proteins (PBPs) with approximate molecular sizes of 94, 82, 52, and 37 kDa were detecte...

Bicifadine [DOV 220,075; (+/-)-1-(4-methylphenyl)-3-azabicyclo[3.1.0]-hexane HCl)] is a non-narcotic analgesic that is effective in animal models of acute and chronic pain. In this study, the pharmacokinetics, disposition, and metabolism of bicifadine were determined in male and female mice, rats, and cynomolgus monkeys following single oral and i.v. doses. [(14)C]Bicifadine was well absorbed i...

Two methods to reduce N-alkyl lactams to the corresponding cyclic amines using 9borabicyclo[3.3.1]nonane (9-BBN) and lithium aminoborohydride (LAB) reagents are reported. The lactam reductions required 2.2 molar equivalents of 9-BBN or 1.5 molar equivalents of LAB reagent and were complete within two hours in refluxing THF (65 °C). Reductions with these reagents are chemoselective and complemen...

UNLABELLED The objectives of this study were to learn about the characteristics and rules of the occurrence of adverse reactions caused by lactam antibiotics and provide a reference for clinical drug use. METHODS A retrospective study was made to analyse the 113 case reports of adverse reactions caused by β-lactam antibiotics collected in our hospital between 2007 and 2009. RESULTS 113 case...

The synthesis (and full spectroscopic and crystallographic characterization) of new classes of bioorganometallic Ir- and Rh-complexes having β-lactam containing ligands has been achieved in three steps starting from simple precursors. The procedure for preparing these bioorganometallic compounds uses β-lactams having a phenylpyridyl moiety attached to the C4, N1 or C4 and N1 positions simultane...

With the goal of developing a modular approach leading to different indoline alkaloid natural-product-like tricyclic derivatives having an unsaturated lactam (see compounds 13, 14, and 16), an aminoindoline-based bicyclic scaffold 10 was obtained from 9. The selective deprotection of the indoline NTeoc or benzylic NHAlloc in compound 10, followed by N-acryloylation and then subjection to a ring...