Abstract

This thesis work encompasses the design, synthesis, and profiling of novel ligands (modulators) binding to an important molecular target, α7 nicotinic acetylcholine receptor (nAChR), which belongs to the ligand gated ion channel group of transmembrane ion channel proteins. Cellular signaling mediated by the α7 receptor is involved in homeostasis of various physiological systems and therefore is considered a crucial target for drug discovery. This work also includes development of novel methodologies in accelerating lead optimization through iterative/parallel synthesis of biologically relevant tetrahydroquinoline and unsymmetrical urea scaffolds using modern technologies such as the microwave synthesizer to significantly enhance the efficiency of the reaction by with improved yield and reduced reaction time.

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