Synthesis and Activity of Pyrimidinylpropenamide Antibiotics: The Alkyl Analogues of Sparsomycin

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.

• total synthesis
• src ^ts-NRK cell
• sparoxomycin A1
• pyridinylpropenamide antibiotic
• structure-activation relationship