Rational design and synthesis of quinazoline derivatives

Year 2021, Volume: 51 Issue: 1, 50 - 58, 30.04.2021

Fatimah Alkharaz Zead Abudayeh Qais Abualassal Loay Hassouneh

Abstract

Background and Aims: Alzheimer's disease is a neurodegenerative disorder in which the death of brain cells causes memory loss and cognitive decline. It is one of the leading causes of mortality worldwide. Several different hallmarks of the disease have been reported such as low levels of acetylcholine, deposits of β-amyloid around neurons, hyperphosphorylated tau protein, oxidative stress, etc. Pharmacotherapy for this disease currently depends on using acetylcholinesterase inhibitors and N-methyl-D-aspartate receptor antagonists. They provide only symptomatic relief and mostly targets cognitive revival. Quinazoline derivatives were recently reported as being a valuable template in the treatment of many neurodegenerative disorders. Quinazoline based compounds were declared as being potential anti AD agents. This research focuses on the synthesis of novel quinazoline derivatives 3 and 4. Methods: Novel quinazoline derivatives 3 and 4 were synthesized starting from 2-(methylamino)benzamide by consecutive steps. The structures of these compounds have been characterized using different analytical and spectral methods: TLC, GC-MS, 1H-NMR and 13C-NMR. Results: This study revealed the synthesis of the novel compounds 3 and 4 with excellent yields equalling 97% and 73.1% respectively. Conclusion: Novel quinazoline derivatives compounds 3 and 4 were obtained. These compounds might be promising lead compounds for potential poly-functional anti-Alzheimer's agents in future work.

Keywords

Quinazoline derivatives, Synthesis, Reaction conditions

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