Parallel solution-phase synthesis and general biological activity of a uridine antibiotic analog library.
作者： Omar Moukha-chafiq , Robert C. Reynolds
DOI: 10.1021/CO4001452
关键词:
摘要: A small library of ninety four uridine antibiotic analogs was synthesized, under the Pilot Scale Library (PSL) Program NIH Roadmap initiative, from amine 2 and carboxylic acids 33 77 in solution-phase fashion. Diverse aldehyde, sulfonyl chloride, acid reactant sets were condensed to 2, leading after acid-mediated hydrolysis, targeted compounds 3–32 good yields high purity. Similarly, treatment with diverse amines sulfonamides gave 34–75. The coupling amino terminus d-phenylalanine methyl ester free 5′-carboxylic moiety followed by sodium hydroxide led analog 77. Hydrolysis this material 78. intermediate served as precursor for preparation novel dipeptidyl 79–99 through peptide reactions reactants. None described show significant anticancer or antimalarial acivity. number samples exhibited a variety pro...
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