Oxadiazoles as potential drugs III.

Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Title of diploma thesis: Oxadiazoles as potential drugs III. Student: Michaela Lukáčová Supervisor: PharmDr. Marta Kučerová, Ph.D. Theoretical part of this diploma thesis summarises biological activity of 1,2,4-oxadiazoles, while focusing primarily on their antimycobacterial, antibacterial and antifungal effects. 1,2,4-Oxadiazoles are compounds with versatile biological applications, therefore their antioxidant, antiinflammatory, analgesic and cytostatic activity is also mentioned. Based on the facts in the theoretical part, it is perceptible, that 1,2,4-oxadiazoles are substances with great therapeutical potential not only for the treatment of tuberculosis, but also many other diseases. Thus, the experimental part of this work is focused on the synthesis of 5-substituted 3-pyrazinyl-1,2,4-oxadiazoles followed by evaluation of their antibacterial, antifungal and most importantly antimycobacterial activity. Synthesic procedure for each compound is also included. Nine compounds were successfully synthesized, six of them were prepared by reaction of N'-hydroxypyrazine-2-carboximidamide with different carboxylic acid anhydrides and three of them by reaction of..