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ACS Comb Sci. 2013 Mar 11;15(3):147-52. doi: 10.1021/co300127z. Epub 2013 Feb 11.

Parallel solution-phase synthesis of an adenosine antibiotic analog library.

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1
Southern Research Institute, Drug Discovery Division, Birmingham, AL 35205, USA. moukhachafiq@southernresearch.org

Abstract

A library of eighty one adenosine antibiotic analogs was prepared under the Pilot Scale Library Program of the NIH Roadmap initiative from 5'-amino-5'-deoxy-2',3'-O-isopropylidene-adenosine 3. Diverse aldehyde, sulfonyl chloride and carboxylic acid reactant sets were condensed to 3, in solution-phase fashion, leading after acid-mediated hydrolysis to the targeted compounds in good yields and high purity. No marked antituberculosis or anticancer activity was noted on preliminary cellular testing, but these nucleoside analogs should be useful candidates for other types of biological activity.

PMID:
23398694
PMCID:
PMC3652606
DOI:
10.1021/co300127z
[Indexed for MEDLINE]
Free PMC Article
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