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Abstract

A FACILE SYNTHESIS OF TRIAZOLOQUINAZOLINONE DERIVATIVES AS POTENTIAL Α-GLUCOSIDASE INHIBITORS

Suresh Poudapally, Venkateshwarlu Gurram, Chiranjeevi Thulluri, Pavan Kumar Machiraju, Anji Karun Mutha, Subhabrata Sen* and Vidya Katangoor*

ABSTRACT

In continuation of our efforts to develop a lead antidiabetic compound, a series of eighteen novel triazoloquinazolinone derivatives have been synthesized and screened against α-glucosidase. The binding mode of the compounds at the active site of α-glucosidase was explored using Glide docking method. 6-Bromo-2,3-disubstituted quinazoline-4(3H)- one analogues are readily converted to the amino derivatives via Buchwald amination that upon diazotization with t-BuONO and TMSN3 yield the stable C-6 azido derivatives. Screening of conditions for the ligation of the azido quinazolinones with alkynes showed that CuSO4 in t-BuOH/H2O is optimal, yielding C-6 modified 1,2,3- triazolyl quinazolinones in 70−82% yields (eighteen compounds). Based on the interaction profile and docking score, all these compounds were selected for in vitro enzymatic screening. Eight of these eighteen compounds showed <20 μM activity against α-glucosidase and amongst these, compound six showed the highest inhibition, with an IC50 of 0.48 μM. In silico analysis was utilized to evaluate the diversity of the set of compounds against shape space (PMI), and relevant drug like properties.

Keywords: Triazoloquinazolinones, Amination, Azide formation, Click chemistry, Docking studies, ?-Glucosidase inhibitors.


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