Materials Science and Chemistry

Biography

Biography: Nana Gorgaslidze

Abstract

Modification of steroids with pharmacophores in order to discover new highly active compounds is a critical problem.  Peptides and proteins play an important role in biological and physiological processes and combinations of amino acids, peptides and steroids have given rise to an interesting class of biologically relevant compounds. Oximes have been evaluated for potential cytotoxicity and oxime derivatives of steroids that have been reported to exhibit antibacterial, anti-inflammatory and anti-cancer activities. In particular, amino acids have been coupled with steroids with the aim of preparing potential therapeutic agents that exhibit lower toxicity whilst retaining the original activity of the parent compound. In the pharmacological perspective, the combination of two important systems in one molecule encourages increasing the biological activity; accordingly the synthesis of steroidal peptides becomes interesting. The derivatives of different oximes modified by amino acids are noteworthy. Despite steroidal oximes being biologically highly active compounds, examples of modification similar to these compounds cannot be found in the literature. In order to synthesize biologically active compounds, O-acylation of 20-hydroximino-5α-pregn-16-en-3β-ole, 3β-acetoxy-20-hydroximino-5α-pregn-16-ene and 17-hydroximino-5α-androstan-3β-ole  with N-protected amino acids  (N-Cbz-L-Ala-Bt, N-Cbz-L-Val-Bt, N-Cbz-L-Phe-Bt and N-Cbz-L-Ala-L-Val-Bt)  have been carried out and their antiviral activities have been studied.