Search

Novel structural analogs of isothiobarbamine, which differ from the prototype scaffold by the substituent at position 2 of the pyrimidine heterocycle, were for the first time synthesized and characterized. Data acquired in pharmacological experiments in vivo revealed that compounds 1b—d and 10 increase physical productivity, whereas compounds 1c and 10 exhibit a nootropic effect, compound 8a shows a psychostimulating effect, and compound 1b exhibits anxiolytic properties. The results reported herein indicate that the drug discovery based on new structural analogs of isothiobarbamine is promising since it may lead to drugs for the prevention and treatment of asthenia (chronic fatigue syndrome). [ABSTRACT FROM AUTHOR]

The review summarizes information on cyclopropane as an independent pharmacophore group and as a fragment for modification of pharmacological activity level of medicines used in practice. The advantages of a cyclopropane fragment over its bioisosteres are that, on the one hand, this fragment imposes conformational rigidity on the molecules of physiologically active compounds and, on the other hand, the replacement of acyclic terminal and “linker” groups with a cyclopropane fragment increases the metabolic stability of the target structures and extends the scope of their therapeutic action. [ABSTRACT FROM AUTHOR]