Many terpenes exhibit various biological activities. In a series of recent articles, it has been reported on the appearance of new biological properties or intensification of the original activity that accompanies the introduction of heterocyclic fragment in the molecules of native terpenoids. Therefore, the synthesis of heterocycle-containing terpenic compounds is of great interest for further bio-activity studies. Present communication put into discussion the recently elaborated methods for preparation of some new biologically active compounds with norlabdane and heterocyclic structural units. Preparation of a series of new tetranorlabdane compounds with triazole, oxadiazole, thiadiazole, and diazine fragments, from local and renewable raw materials is reported. The newly synthesized compounds exhibit selective biological activity and low toxicity due to the natural origin of these substances. A comprehensive study of the synthesis and structure of new tetranorlabdane compounds with diazine skeleton is also presented. The first synthesis of tetranorlabdane compounds with diazine skeleton is discussed. At the same time, an efficient way for the one-pot bis-acylation of 2-aminopyrimidine is reported. Amides of Δ8, 13-bicyclohomofarnesenic acid containing 1, 2, 4-triazole and carbazole rings were synthesized in eight steps from sclareolide. Compounds were prepared by coupling the corresponding acid chloride with the heterocyclic amines: 3-amino-1, 2, 4-triazole and N-aminocarbazole. The results of investigations devoted to the synthesis of new homodrimane compounds containing thiadiazole and oxadiazole structural units are reported. The homodrimane derivatives with thiadiazole units were prepared from the intermediate hydrazide, which was treated with TMTD (tetramethyl thiuram disulfide). The homodrimane derivatives with oxadiazole units were obtained from the intermediate hydrazide upon its interaction with CDI (1, 1′-carbonyldiimidazole). All the newly-obtained compounds were identified and characterized by IR- and 1H, 13C NMR- spectroscopic methods, their structures being confirmed by single crystal X-ray diffraction. All compounds were tested for antibacterial and antifungal activity, some of them have shown quite pronounced activity against gram positive and gram negative bacteria and fungal strains.