thionyl chloride (or oxalyl chloride) has been used as an efficient and cheap acid activator for one-pot synthesis of β-lactams in good to excellent yields by reaction between imines and acids in the presence of triethylamine at room temperature.

BACKGROUND Systemic corticosteroids have anti-inflammatory effects, whereas macrolides also have immunomodulatory activity in addition to their primary antimicrobial actions. We aimed to evaluate the potential interaction effect between corticosteroids and macrolides on the systemic inflammatory response in patients with severe community-acquired pneumonia to determine if combining these two im...

Methicillin-resistant Staphylococcus aureus (MRSA) has acquired the mecA gene encoding a peptidoglycan transpeptidase, penicillin binding protein 2a (PBP2a), which has decreased affinity for β-lactams. Quickly spreading and highly virulent community-acquired (CA) MRSA strains recently emerged as a frequent cause of infection in individuals without exposure to the health care system. In this stu...

Bacterial resistance to standard (i.e., β-lactam-based) antibiotics has become a global pandemic. Simultaneously, research into the underlying causes of resistance has slowed substantially, although its importance is universally recognized. Key to unraveling critical details is characterization of the noncovalent interactions that govern binding and specificity (DD-peptidases, antibiotic target...

The fates of BlaI, the gene repressor protein for the bla operon, BlaR1, the β-lactam sensor/signal transducer, and PC1 β-lactamase in four strains of Staphylococcus aureus upon exposure to four different β-lactam antibiotics were investigated as a function of time. The genes for the three proteins are encoded by the bla operon, the functions of which afford inducible resistance to β-lactam ant...

Introduction An economical way to obtain optically active β-lactam derivatives is the use of amino acids as chiral auxiliaries in Staudinger reaction (Bose et al., 1985). This strategy has been used for asymmetric synthesis of bicyclic β-lactam compounds, such as 2-isocephems, from threonine (Tenneson and Belleau, 1980). In addition, β-lactams obtained by this method are useful as versatile int...

OBJECTIVES plasmid pB1000 bearing bla(ROB-1) is responsible for high-level β-lactam resistance in Haemophilus influenzae as well as in Pasteurella multocida and Haemophilus parasuis isolates from Spain. Here, we explore the presence of ROB-1 in Italy and investigate the relative contribution of penicillin-binding protein 3 (PBP3) mutations and ROB-1 to the β-lactam resistance phenotype in H. in...

OBJECTIVES Enterococci are an important cause of nosocomial and community-acquired infections, with bacteraemia being one of the most common presentations. Although inappropriate antimicrobial therapy has been associated with poorer outcomes in Enterococcus faecalis (EF) bacteraemia, the impact of antimicrobial choice, namely β-lactam versus glycopeptide therapy, has not been well described. We...

The manuscript pertains to the synthesis of urea/oxalamide tethered β-lactam-7-chloroquinoline conjugates with well modulated chain lengths and their antimalarial evaluation. The results reveal the dependence of activity profiles on the N-1 substituent of the β-lactam ring, the nature of the linker as well as the length of the alkyl chain. The most potent of the tested compounds showed an IC50 ...