Macrolide 2'-phosphotransferase [MPH(2')] transfers the gamma phosphate of ATP to the 2'-OH group of macrolide antibiotics. The role of aspartic acids in the putative ATP-binding site of MPH(2')II was investigated through the substitution of alanine for aspartate by site-directed mutagenesis. D200A, D209A, D219A, and D231A mutant strains were unable to inactivate the substrate oleandomycin, whi...

Macrolide antibiotics are widely used for a range of indications, including pneumonia. Both high-level and low-level resistance to macrolides is increasing in pneumococci globally. Macrolide resistance in pneumococci is of limited clinical relevance where ß-lactams remain the mainstay of treatment, such as for moderate/severe pneumonia; however, data suggest that macrolides may not be able to b...

Ten strains of beta-hemolytic streptococci were tested for elimination of resistance to macrolide antibiotics, tetracycline, and chloramphenicol. Six of the strains lost resistance after cultivation at 41 C or addition of acriflavine (0.2 mug/ml). These results suggest that determinants governing resistance to these antibiotics are located on extrachromosomal genetic elements (plasmids) that ar...

Macrolides are widely used as antibacterial drugs. Clinical and experimental data, however, indicate that they also modulate inflammatory responses, both contributing to the treatment of infective diseases and opening new opportunities for the therapy of other inflammatory conditions. Considerable evidence, mainly from in vitro studies, suggests that leukocytes and neutrophils in particular, ar...

Aminoglycosides Amikacin Framycetin Sulphate Gentamicin Sulphate Kanamycin Sulphate Lincomycin Neomycin Spectinomycin Tobramycin PET imaging tracer FDG Macrolide antibiotics Azithromycin Azaerythromycin Clarithromycin Erythromycin Roxithromycin Bioanalysis of pharmaceutics Acetaminophen Artemisinin Dihydro-artemisinin Artemether Etoposide 8-OH-DPAT mesna BNP7787 Vincristine Application Note Bio...

Three novel 36-membered macrolide antibiotics, RS-22A, B and C produced by Streptomyces violaceusniger have been isolated. These antibiotics were purified from an acetone extract of the mycelia followed by butanol extraction, centrifugal partition chromatography and HPLC. RS-22A, B, C showed antimicrobial activity against fungi and Gram-positive bacteria.

Synthesis and biological properties of a number of amides of polyene macrolide antibiotic aureofacin obtained in the reaction of the antibiotic with various glycine esters are described.