Preparation of beta-aminomethyl-beta-benzoylpropionic acids and related cis beta-aminomethyl-gamma-phenyl-gamma-butyrolactones as potential antibacterial agents.

The synthesis of beta-aminomethyl-beta-benzoylpropionic acids (V) and beta-aminomethyl-gamma phenylbutyrolactones (VI) is described. The cis stereochemistry of compounds VI was unambiguously established by NOE experiments carried out with Vla. Antibacterial activity was studied; MIC of each derivate was determined by agar dilution in Muller-Hinton medium and application of Steers' replicator.