European Journal of Chemistry

Quinazolin derivatives as emerging alpha-glucosidase inhibitors

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Ashok Reddy Ankireddy
Rambabu Gundla
Tuniki Balaraju
Venkanna Banothu
Krishna Prasad Gundla
Uma Addepally
Jithendra Chimakurthy

Abstract

A series of C-7 substituted-2-morpholino-N-(pyridin-2-ylmethyl)quinazolin-4-amine have been synthesized and biochemical assay was examined against α-glucosidase function inhibition activity. A structure activity and structure property relationship study was experimented to surface the new hit compound. This study led to the identification of C-7substituted quinazolines with minimum inhibitory concentrations (MICs) in the preffered micromolar range in addition with interesting physicochemical properties. Biological evaluation yielded eight analogs which rose with significant α-glucosidase inhibition potency (IC50 values < 2 μM, where reference compound (Acarbose) potency value is IC50 = 0.586 uM) and could be promising candidates for further lead optimization.


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Ankireddy, A. R.; Gundla, R.; Balaraju, T.; Banothu, V.; Gundla, K. P.; Addepally, U.; Chimakurthy, J. Quinazolin Derivatives As Emerging Alpha-Glucosidase Inhibitors. Eur. J. Chem. 2018, 9, 322-330.

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Supporting Agencies

Science and Engineering Research Board (SERB) India and Gandhi Institute of Technology and Management (GITAM) University School of Science, Departmet of Chemistry, Hyderabad
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