Date Approved

5-1-2018

Embargo Period

5-2-2018

Document Type

Thesis

Degree Name

MS Pharmaceutical Sciences

Department

Chemistry and Biochemistry

College

College of Science & Mathematics

First Advisor

Jonnalagadda, Subash

Second Advisor

Ramanujachary, Kandalam

Third Advisor

Wu, Chun

Subject(s)

Pharmaceutical chemistry; Organic compounds--Synthesis

Disciplines

Medicinal and Pharmaceutical Chemistry | Pharmacy and Pharmaceutical Sciences

Abstract

Multicomponent coupling reactions (MCRs) have been known for a long time and one such reaction that utilizes isocyanides is Passerini reaction. It is a powerful tool to synthesize libraries of different compounds. Azaheterocyclic compounds play an important role in medicinal chemistry. Motifs such as imidazoles, piperazines, pyrazoles, pyridines, triazoles, etc. are routinely observed in several compounds of pharmacological interest. Several natural products also contain these motifs in them. We have undertaken a library synthesis of heterocyclic molecules driven by our group's long-standing interest of synthesizing medicinally relevant small molecules employing green chemistry techniques.

This thesis details our efforts on the development of novel synthetic methodologies for the synthesis of functionalized azaheterocyclic compounds as potential anti-cancer agents. We initiated the synthesis of these compounds employing Passerini reaction as the key step. The biological evaluation of these synthetic derivatives showed some promise as anti-cancer agents.

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