Following the principles of green chemistry, cardanol derivatives have been used as renewable, low-cost, and available natural starting materials to construct a variety of protected and unprotected amino acids derivatives. The reaction of cardanol derivatives with different phthaloylamino acids including glycine, alanine, phenylalanine, and valine in the presence N,N’-dicyclohexylcarbodiimide (DCC) as coupling reagent afforded high yields of the target compounds. Deprotection of phthaloylamino acids derivatives was achieved by heating with hydrazine hydrate. The chemical structures of all products were confirmed by spectral data (IR, MS, 1H NMR, 13C NMR) and elemental analyses. Antibacterial evaluation of the synthesized products was performed, which exhibited potent to weak activity in comparison with a standard drug.