In the last 20 years there has been a significant increase in interest in the structure of oxadiazole derivatives, especially 3-acetyl-1,3,4-oxadiazolines. It is known that these derivatives possess: antibacterial, antifungal, antitubercular, antiprotozoal, anticancer and anti-inflammatory activity. Therefore, many medicinal chemists choose 3-acetyl-1,3,4oxadiazoline scaffold for the synthesis of new potentially active substances with a better effectiveness and less toxicity. This article is a literature review since 2000 presenting new derivatives with proven antimicrobial and antiprotozoal activity, containing in its structure a 3-acetyl-1,3,4-oxadiazoline system.