A series of novel 3-[ N, N-bis(2-hydroxyethyl)-amino]-chalcone derivatives 3a-3j were synthesized by the aldol condensation of [ N, N-bis(2-hydroethyl)-3-amino]-acetophenone 2 with aromatic aldehydes. Their structures were further confirmed by ESI-HRMS, H NMR, IR and elemental analysis. X-ray analysis reveals crystal 3b is a monoclinic system with P2/ n space group. The antimicrobial activities of the newly synthesized chalcones in vitro were evaluated and the results indicated that most compounds presented moderate to good antimicrobial activities, especially the antifungal capability. Compounds 3a, 3d, 3f and 3g revealed obvious potency against Candida albicans with MIC values of 32 μg/mL, which were better compared with others. [ABSTRACT FROM AUTHOR]