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Research & Reviews: Journal ofPharmaceutical Analysis | ISSN : 2320-0812
Euro Pharma Chemistry & Future Pharma 2019
June 27-28, 2019 | Amsterdam, Netherlands
12th World congress on
Joint Event
4
th
Pharmaceutical Chemistry Conference Future Pharma
Volume 08
Synthesis, structural characterizationanddocking studies of sulfamoyl-
phenyl acid esters as dipeptidyl peptidase-IV inhibitors
D
iabetes mellitus is a major worldwide health concern that has several
serious complications including retinopathy, neuropathy, nephropathy and
macrovascular diseases. Dipeptidyl peptidase-IV (DPP-IV) inhibitors, gliptins,
are a new class of antidiabetic agents that potentiates the action of incretins
in decreasing the blood glucose levels. In the present study, synthesis and
characterization of a series of 10 N4-sulfonamido-acrylic and phthalamic acid
methyl esters (3a-e and 5a-e) were achieved.
In vitro
anti-DPP-IV activity of
the synthesized compounds was evaluated, where compound 3b demonstrated
the best activity with a percent (%) inhibition of 41.7 at 10 μM concentrations
and an IC50 of 23.9 μM. Moreover, Glide docking experiments revealed that our
targeted compounds accommodate the binding site of DPP-IV and tend to form
H-bonding with the backbones of R125, E206, S209, D545, K554, W629, Y631
and G632. Modeling findings recommend the attachment of bulky hydrophobic
group on the ester side of the structure in addition to harboring extra aromatic
rings that might be beneficial for better binding interaction and biological activity.
Biography
Reema Abu Khalaf currently is an Associate Professor of Medicinal Chemistry and Drug
Discovery, at Faculty of Pharmacy, Al-Zaytoonah University of Jordan. She has completed
her BSc in Pharmacy, MSc in Pharmaceutical Sciences, and PhD in Medicinal Chemistry and
Drug Discovery at The University of Jordan. She got the Distinguished Researcher Award
from Al-Zaytoonah University of Jordan, Jordan, 2012. Currently, her researches focus on
the design and synthesis of new dipeptidyl peptidase-IV inhibitors that can serve as potential
hypoglycemic agents. Furthermore, the design and synthesis of new inhibitors of cholesteryl
ester transfer protein as anti-hyperlipidemic agents. She has published more than 20 papers
in reputed journals.
reema.abukhalaf@zuj.edu.joReema Abu Khalaf et al., Pharmaceutical Analysis 2019, Volume 08
Reema Abu Khalaf
Al-Zaytoonah University of Jordan, Jordan
Co-Authors
Dima Sabbah, Eveen Al-Shalabi, Iyad
Al-Sheikh, Ghadeer Albadawi
and
Ghassan Abu Sheikha
Al-Zaytoonah University of Jordan, Jordan