Vinod Sukanth Kumar Pallabothula
Didactic Department of Organic Chemistry and Chemical Technology
Research Group: Laboratory of Natural Products Chemistry
Poster Title: Synthesis and biological evaluation of singlet oxygen generated melatonin derivative containing suberic acid moiety
Student name: Vinod Sukanth Kumar Pallabothula
Promotor: Dr Anna Zawadzka
Alzheimer’s Disease is serious issue accelerating day by day with high probability towards its procurement in humans1. Cholinesterase inhibition is the main crucial possibility along with its ground-breaking drugs available in the market for the treatment. However, these compounds are not reliable2. The present research focuses on synthesis of potent cholinesterase inhibitors. Due to the scientific discovery of more than one active sites of cholinesterase enzyme3, dimers of melatonin and pyrroloindole derivatives connected by alkyl chain are synthesised4, 5. These compounds have undergone for biological evaluation following Ellman’s method6 on both human acetylcholinesterase and human butyrylcholinesterase enzymes. The melatonin homodimer is highly selective to butyrylcholinesterase inhibition but also showed a significant effect on acetylcholinesterase inhibition. These dimers are potential candidate for multifunctional ligands due to the presence of a melatonin fragment- a good antioxidant.
Literature:
[1] Martone, R.; Piotrowski, N. Magill’s Medical Guide [Online Edition]. 2013. 8.
[2] Lau, L-F.; Brodney, MA. (Ed.). Springer, Berlin 2008.
[3] Tripathi, A.; Srivastava, U.C. Annals of neurosciences. 2008. 15. 4.
[4] Siwicka, A.; Molęda, Z.; Wojtasiewicz, K.; Zawadzka, A.; Maurin, J. K.; Panasiewicz, M.; Pacuszka, T.; Czarnocki, Z. J. Pin. Res. 2008. 45. 40–49.
[5] Zawadzka, A.; Łozińska, I.; Molęda, Z.; Panasiewicz, M.; Czarnocki, Z. J. Pin. Res. 2013. 54. 435-441.
[6] Ellman, GL.; Courtney, KD.; Anders, V.; Feartherstone, RM. Biochem Pharmacol. 1961. 7. 88–95.