The aim of the doctoral thesis was to develop high affinity agonists of hydroxycarboxylic acid receptor 2. Conformational restriction approach of known agonists, pharmacophore model development, and bioisosteric replacement strategy were used to design new ligands. Structure-activity relashionships of synthesized ligands and their binding to plasma proteins were analyzed. Methods for the preparation of hydroxycarboxylic acid receptor 2 agonists (E)-2-(3-(arylacrylamido)cyclohex-1-enecarboxylic acids, 2-(3-arylpropiolamido)cyclohex-1-enecarboxylic acids un 2-(5-arylpent-4-ynamido)cyclohex-1-enecarboxylic acids have been developed.