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Design, Synthesis, and Biological Evaluation of Novel Quinazoline Clubbed Thiazoline Derivatives
Author(s) -
Ali Zulphikar,
Akhtar Md J.,
Siddiqui Anees A.,
Khan Ahsan A.,
Haider Md R.,
Yar Mohammad S.
Publication year - 2017
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201600298
Subject(s) - thiazoline , chemistry , quinazoline , combinatorial chemistry , selectivity , docking (animal) , stereochemistry , chemical synthesis , in vitro , ic50 , biochemistry , catalysis , medicine , nursing
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 (IC 50 = 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.