One-pot synthesis of novel tert-butyl-4-substituted phenyl-1H-1,2,3-triazolo piperazine/piperidine carboxylates, potential GPR119 agonists.

Autor: Bashetti N; Department of Chemistry, Koneru Lakshmaiah Education Foundation, Andhra Pradesh 522502, India., Shanmukha Kumar JV; Department of Chemistry, Koneru Lakshmaiah Education Foundation, Andhra Pradesh 522502, India., Seelam NV; Department of Chemistry, Koneru Lakshmaiah Education Foundation, Andhra Pradesh 522502, India., Prasanna B; Department of Chemistry, Koneru Lakshmaiah Education Foundation, Andhra Pradesh 522502, India., Mintz A; Department of Radiology, Columbia University Medical Center, New York, NY, USA., Damuka N; Department of Radiology, Wake Forest School of Medicine, Winston Salem, NC, USA., Devanathan S; Medical Guidance Systems LLC, St. Louis, MO, USA., Solingapuram Sai KK; Department of Radiology, Wake Forest School of Medicine, Winston Salem, NC, USA. Electronic address: ksolinga@wakehealth.edu.
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2019 Dec 01; Vol. 29 (23), pp. 126707. Date of Electronic Publication: 2019 Sep 16.
DOI: 10.1016/j.bmcl.2019.126707
Abstrakt: We have synthesized a new series of 1,2,3-triazolo piperazine and piperidine carboxylate derivatives using a simple and one-pot click chemistry with significantly reduced reaction times (~5 min) and enhanced reaction yields (~95-98%). The fourteen novel compounds thus synthesized were tested for ability to target GPR119, a G-protein coupled target receptor that plays critical role in regulation of type-2 diabetes mellitus. Four analogs (3e, 3g, 5e and 5g) demonstrated similar or better EC 50 values over previously reported AR231453 activity towards GPR119.
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Databáze: MEDLINE
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