533914-89-5Relevant academic research and scientific papers
MACROCYCLIC COMPOUNDS AND METHODS OF MAKING AND USING THE SAME
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Page/Page column 227, (2010/02/14)
The present invention provides macrocyclic compounds useful as therapeutic agents. More particularly, these compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents.
Design, synthesis and ribosome binding of chloramphenicol nucleotide and intercalator conjugates
Johansson, Dorte,Jessen, Carsten H.,Pohlsgaard, Jacob,Jensen, Kenneth B.,Vester, Birte,Pedersen, Erik B.,Nielsen, Poul
, p. 2079 - 2083 (2007/10/03)
Molecular modelling based on X-ray structures of the antibiotic drug chloramphenicol bound in a bacterial ribosome has been used for design of chloramphenicol derivatives. Conjugates of the chloramphenicol amine through appropriate linkers to either a pyrene moiety or to a mono- or dinucleotide moiety were designed to improve binding to ribosomes by providing specific interactions in the peptidyl transferase site or to the P-loop in the ribosome. Specific binding of the conjugates were investigated by footprinting analysis using chemical modifications of accessible nucleotides in ribosomal RNA. The pyrene chloramphenicol conjugate shows enhanced binding to the chloramphenicol binding site compared to the native chloramphenicol, whereas the four nucleotide conjugates could not be shown to bind to the chloramphenicol binding site or to the P-loop.
An Approach to Enhance Specificity against RNA Targets Using Heteroconjugates of Aminoglycosides and Chloramphenicol (or Linezolid)
Lee, Jongkook,Kwon, Miyun,Lee, Kyung Hyun,Jeong, Sunjoo,Hyun, Soonsil,Shin, Kye Jung,Yu, Jaehoon
, p. 1956 - 1957 (2007/10/03)
We describe the design and synthesis of new heterodimeric conjugates, which are comprised of a neomycin B (Neo) stem-binding component and a chloramphenicol (Cam) or linezolid (Lnz) loop-binding component. Some of the heterodimeric conjugates display enha
