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Synthesis and Activity of Pyrimidinylpropenamide Antibiotics: The Alkyl Analogues of Sparsomycin |
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| Abstract: | Facile syntheses of sparsomycin (3) and its four analogues (4-7) based on diastereoselective oxidation of sulfide, sulfenylation, and coupling of 6-methyluracylacryllic acid with monooxodithioacetal amine, are described. Studies on the biological activity of morphological reversion on src ts-NRK cells were also carried out. |
| Keywords: | total synthesis src ts-NRK cell sparoxomycin A1 pyridinylpropenamide antibiotic structure-activation relationship |