Document Type and Release Option
Thesis (open access)
Dr. Abid Shaikh
Structure activity relationship (SAR) studies are performed in order to identify the core structure that is responsible for the biological activity of an organic molecule. Recently, we have synthesized a drug prototype which contains several functional groups, such as an alcohol, an ester, a fluorine, and an aromatic ring. While studying in vivo toxicity of this molecule in zebrafish (Danio rerio) embryo, we observed that it has a unique biological activity that causes a sudden inactivity in embryo movement. Continued investigation revealed that this molecule blocks sodium channels in neurons causing a temporary anesthesia in Danio rerio embryo. The biological activity in zebrafish was performed with Dr. Sittaramane. We have also observed that after transferring the embryo to fresh water, the embryo resumed normal behavior. As our next step, we would like to synthesize a variety of structural analogs and determine their activity. The ultimate goal of this project was to develop effective methods of synthesizing various molecules that have one of the functional groups removed in order to identify its role in biological activity. All products and intermediates will be fully analyzed using NMR, IR and Mass spectrometer analysis. Further structural modifications may be required depending on the activity findings. After successful synthesis of the proposed molecules, Dr. Sittaramane and I performed in vivo activity determination.
Smeyne, Dylan, "Structure activity relationship (SAR) studies of neurotoxin quinoline-derivatives" (2020). Honors College Theses. 484.