The project
Naturally occurring or lab synthesized heterocycles dominate pharmaceutical products. In 2015, 70% of the top 20 best-selling drugs (by revenue), and 65% of the compounds on the World Health Organization’s (WHO’s) essential medicines list were heterocyclic. In addition, most of today’s pharmaceuticals contain heterocycles that arise from a close study of the biological properties of Small Molecule Natural Products (SMNPs). The study of SMNPs provides compounds of often unusual structural diversity and complexity. Naturally produced SMNPs can often be isolated only in small quantities making studies on their biological properties difficult, expensive and often ecologically unsound. Furthermore, SMNPs can show undesirable toxicities or lack specificity that limit their usefulness.
Canthin-4-ones is a limited studied class of SMNPs. Antibacterial activities for the canthin-4-ones were only recently reported in 2016 by Bracher et al.5 Two canthin-4-ones showed good antimicrobial activity (agar diffusion assay) against Streptococcus entericus comparable to the commercial drug tetracycline. The limited data in the literature for the antimicrobial efficacy of canthin-4-ones, opens up a huge space for exploration that with the combination of novel structures will provide opportunities for new findings. Nevertheless, for the study of these materials a general and high yielding synthesis is on demand.
In this project we will aim the development of high yielding and general synthesis of canthin-4-ones.
Canthin-4-ones is a limited studied class of SMNPs. Antibacterial activities for the canthin-4-ones were only recently reported in 2016 by Bracher et al.5 Two canthin-4-ones showed good antimicrobial activity (agar diffusion assay) against Streptococcus entericus comparable to the commercial drug tetracycline. The limited data in the literature for the antimicrobial efficacy of canthin-4-ones, opens up a huge space for exploration that with the combination of novel structures will provide opportunities for new findings. Nevertheless, for the study of these materials a general and high yielding synthesis is on demand.
In this project we will aim the development of high yielding and general synthesis of canthin-4-ones.
Meet the team
Dr Maria Koyioni
(Project Coordinator - Special Scientist) |
Prof. Panayiotis A. Koutentis
|
Dr Georgia Zissimou
(Special Scientist - 2 months) |
Panayiota Kelis
(Special Scientist - 10 months) |