title: Design, Synthesis, and Biological Evaluation of Novel Quinazoline Clubbed Thiazoline Derivatives.
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.
authors.affiliation: Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Jamia Hamdard (Hamdard University), Hamdard Nagar, New Delhi, India.
authors.forename: Zulphikar
authors.initials: Z
authors.lastname: Ali
authors.affiliation: Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Jamia Hamdard (Hamdard University), Hamdard Nagar, New Delhi, India.
authors.forename: Md J
authors.initials: MJ
authors.lastname: Akhtar
authors.affiliation: Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Jamia Hamdard (Hamdard University), Hamdard Nagar, New Delhi, India.
authors.forename: Anees A
authors.initials: AA
authors.lastname: Siddiqui
authors.affiliation: Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Jamia Hamdard (Hamdard University), Hamdard Nagar, New Delhi, India.
authors.forename: Ahsan A
authors.initials: AA
authors.lastname: Khan
authors.affiliation: Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Jamia Hamdard (Hamdard University), Hamdard Nagar, New Delhi, India.
authors.forename: Md R
authors.initials: MR
authors.lastname: Haider
authors.affiliation: Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Jamia Hamdard (Hamdard University), Hamdard Nagar, New Delhi, India.
authors.forename: Mohammad S
authors.initials: MS
authors.lastname: Yar
mesh_terms: D000818:Animals; D001786:Blood Glucose / Q000187:drug effects; D054873:Dipeptidyl-Peptidase IV Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004152:Dipeptidyl-Peptidases and Tripeptidyl-Peptidases / Q000037:antagonists & inhibitors*; D015195:Drug Design; D000069476:Linagliptin / Q000494:pharmacology; D062105:Molecular Docking Simulation; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D001786:Blood Glucose; D054873:Dipeptidyl-Peptidase IV Inhibitors; D011799:Quinazolines; D000069476:Linagliptin; D004152:Dipeptidyl-Peptidases and Tripeptidyl-Peptidases
keywords: Antidiabetic; DPP-4 inhibitors; Molecular docking; Quinazoline; Thiazoline