Date Approved

1-22-2021

Embargo Period

1-26-2021

Document Type

Thesis

Degree Name

M.S. Pharmaceutical Sciences

Department

Chemistry and Biochemistry

College

College of Science & Mathematics

Advisor

Ramanujachary, Kandalam

Committee Member 1

Jonnalagadda, Subash

Committee Member 2

Mugweru, Amos

Keywords

Aza Heterocyclic Compounds, Multicomponent coupling reactions, Trisubstituted Imidazoles

Subject(s)

Drug development; Heterocyclic compounds; Imidazoles

Disciplines

Medicinal-Pharmaceutical Chemistry | Pharmacy and Pharmaceutical Sciences

Abstract

Aza heterocyclic compounds are an important class of organic compounds that play a major role in medicinal chemistry. Majority of the heterocyclic motifs such as imidazoles, triazoles, piperazines etc. act as building blocks for synthesizing active pharmaceutical ingredients. Several pharmaceutical drugs include these motifs due to their varying physicochemical properties, which enable them to exhibit wide range of pharmacological activities ranging from anti-fungal, anti-neoplastic, anti-helmintic, anti-microbial etc. Owing to their electron rich ring system, imidazole and piperazine based motifs have become an attractive target for design and development of novel chemical structures as new drugs. In the current study, we have synthesized a series of 2, 4, 5-trisubstituted imidazole-based compounds containing different pharmacophores using multicomponent coupling reactions such as Baylis-Hillman reaction and Debus-Radziszewski reaction. A preliminary report on the structural activity relationship of the synthetic compounds was also obtained based on an in vitro cytotoxicity evaluation against three cancer cell lines.

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