Abstract: A series of benzothiazolylthioacetyl amino acid and peptide derivatives including glycoside, hydrazide and hydrazone moieties were synthesized with the aim of evaluating their antifungal activity. Their chemical structures were confirmed by 1 H NMR, IR, mass spectrometry and elemental analyses. Out of the thirty two tested compounds three derivatives have enhanced activity as fluconazole at 100 ppm and six at 1000 ppm toward Candida albicans whereas, they were actually inactive toward Aspergillus flavus.