Design, Synthesis, and Biological Evaluation of Novel Quinazoline Clubbed Thiazoline Derivatives

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. A novel series of quinazoline clubbed thiazoline derivatives was rationally designed, synthesized and evaluated for their in vitro dipeptidyl peptidase IV (DPP‐4) inhibitory activity, compared to the standard linagliptin. Docking of the most promising compound (4x) into the active site of DPP‐4 reveals its possible binding interactions.