5α-steroidal amines: Synthesis and biological activity

6^th World Congress on Medicinal Chemistry and Drug Design

June 07-08, 2017 Milan, Italy

N Nadaraia, M Merlani, N Barbakadze, N Amiranashvili and M Kakhabrishvili

Tbilisi State Medical University, Georgia

Posters & Accepted Abstracts: Med Chem (Los Angeles)

Abstract :

Steroidal amines are characterized with wide spectrum of pharmacological activities such as antitumor, anti-inflammatory, antibacterial and anti-arrhythmic activity. On the basis of epiandrosterone acetate, product of transformation of tigogenin (isolated from plant Yucca gloriosa), eight possible epimer of 3-amino-17-hydoxy- and 17-amino-3-hydroxy-5�±-androstane have been synthesized and their radioprotective and antiarrhythmic activities have been investigated. Among epimeric aminoalcohols the highest radioprotective activity showed 3�²-amino-5�±-androstan-3�²-ole, while with the highest antiarrhythmic activity is characterized 17�²-amino-5�±-androstan-3�²-ole. Based on these results some conclusion about structure- activity relationship of synthesized compounds could be made. For radioprotective activity more profitable is diaxial orientation of amino- and hydroxy groups; whereas, diequatorial orientation is favorable for the antiarrhythmic activity. Some synthesized of N-alkyl- and N-dialkylamino acetyl derivatives of 17�²-amino-5�±-androststan-3�²-ole and 17�²-amino-5�±-androst-2-ene exhibit antiviral, antitubercular and antitumor activities.

Biography :

N Nadaraia has completed her PhD from Mendeleev Moscow Chemical-Technological Institute. She is a lead research scientist at Tbilisi State Medical University. Her field of interest is a Chemistry and synthesis of biologically active compounds. She is the author of more than 40 papers in reputed journals and has presented at 50 international scientific conferences.

Email: nnadaraia@ymail.com