Synthesis and antibacterial activity of C-6 carbamate ketolides, a novel series of orally active ketolide antibiotics

Bioorganic and Medicinal Chemistry Letters

Volumn 14, Issue 17, 2004, Pages 4495-4499

  Henninger, Todd C ^a   Xu, Xiaodong ^a   Abbanat, Darren ^a   Baum, Ellen Z ^a   Foleno, Barbara D ^a   Hilliard, Jamese J ^a   Bush, Karen ^a   Hlasta, Dennis J ^a   MacIelag, Mark J ^a  

^a JOHNSON AND JOHNSON PHARMACEUTICAL RESEARCH AND DEVELOPMENT   (United States)

Author keywords

Antibiotics; Carbamate; Ketolide; Resistant bacteria

Indexed keywords

AZITHROMYCIN; CARBAMIC ACID DERIVATIVE; ERYTHROMYCIN; KETOLIDE; MACROLIDE; TELITHROMYCIN;

ANTIBACTERIAL ACTIVITY; ARTICLE; CONTROLLED STUDY; DRUG SCREENING; DRUG SYNTHESIS; EPIMERIZATION; IN VITRO STUDY; IN VIVO STUDY; NONHUMAN; STEREOCHEMISTRY;

ADMINISTRATION, ORAL; ANIMALS; ANTI-BACTERIAL AGENTS; CARBAMATES; FEMALE; KETOLIDES; MICE; MICROBIAL SENSITIVITY TESTS;

EID: 3843122210     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.06.045     Document Type: Article

References (24)

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21. The most instructive piece of data was the presence of a NOESY cross-peak between the C-2 and C-5 protons in the minor isomer that was not observed in the major isomer (see Supplementary data). Examination of molecular models suggested reasonable conformations could be generated for the minor isomer, but not for the major isomer, which would place these two protons in sufficient proximity to observe an NOE
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24. 50 ) was calculated using the Logistic routine of the SAS suite of programs