Azoles refers to a big class of heterocyclic compounds that contain non-carbon atom (e.g N, O, S elements) in five-membered ring. Azoles are an important class of heterocycles as a chemical scaffold with interesting biological properties. Hantzsch-Widman nomenclature (a type of systematic chemical nomenclature that used for naming heterocyclic parent) is the origin of their names. Therapeutically some active compounds that contain azole moiety have been reported. Due to the presence of azole moiety in some important drugs, interest in the construction of such moiety (single or fused ring) has been aroused. In this review, recent trends of synthesis of some azole derivatives and their major biological activities will be reviewed.