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Updated: Mar 8, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Design, Synthesis, and Biological Evaluation of Novel Quinazoline Clubbed Thiazoline Derivatives
Zulphikar Ali1, Md J Akhtar1, Anees A Siddiqui1
1Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Jamia Hamdard (Hamdard University), Hamdard Nagar, New Delhi, India.
Abstract:
A novel series of quinazoline clubbed thiazoline derivatives was rationally designed and synthesized. The newly synthesized compounds were evaluated for in vitro dipeptidyl peptidase IV (DPP-4) inhibitory activity. Compounds that showed good to moderate activity were compared using linagliptin as standard. Compound 4x (IC50 = 1.12 nM) exhibited the most promising results. The special chemical feature of compound 4x also imparts good inhibition selectivity for DPP-4 over DPP-8/9. Moreover, docking of compound 4x into the active site of DPP-4 illustrates its possible binding interactions.
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