This paper is part of ongoing research at the Department of Medicinal Chemistry, Faculty of Pharmacy and Biochemistry, University of Zagreb. The research includes the design, synthesis and biological evaluation of novel harmine derivatives as potential antimalarial drugs. The aim of this diploma thesis was the synthesis and characterization of novel harmine urea derivatives comprising mefloquine moiety in their structure. The synthesis began with the transformation of the mefloquine derivative to amine 1. Harmol 2 was generated from harmine, while phenol 7 was generated from 5-methoxytryptamine. Then, harmine, harmol and phenol 7 were converted into amines 3, 5 and 10 using 2-(Boc-amino)ethyl bromide and subsequently, hydrochloric acid. The final products, ureas 12a-c, were synthesized by nucleophilic substitution from amines 3, 5, 10 and amine 1. CDI was used as a coupling reagent. The structures of newly synthesized compounds were confirmed using analytical and spectroscopic methods (IR, 1H and 13C NMR, MS). In addition, melting points were determined for solid compounds. Novel derivatives fulfil some of Lipinski’s and Veber’s criteria for good oral bioavailability of potential drugs. SwissADME web tool predicts poor oral bioavailability as well. The antimalarial and cytostatic activity of the newly synthesized compounds will be examined in further studies.