Activation of the GLP-1 receptor by chloropyrimidine derivatives

The anti-diabetic activities of a series of chloropyrimidine derviatives 2a-k and 4a-k were investigated after they were designed, synthesized, and docked against the GLP-1 receptor target. In comparison to exenatide, which was utilized as a reference drug, the three chloropyrimidine synthesized com...

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Autores principales:	Shaikha S. AlNeyadi, Abdu Adem, Naheed Amer, Mohammad A Ghattas, Noor Atatreh, Alaa A. Salem, Ibrahim M. Abdou
Formato:	article
Lenguaje:	EN
Publicado:	Elsevier 2021
Materias:	Synthesis Type 2 diabetes GLP-1 Pyrimidine Docking Chemistry QD1-999
Acceso en línea:	https://doaj.org/article/abf9bb2a2d3841919333302b3a95cdb0
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spelling	oai:doaj.org-article:abf9bb2a2d3841919333302b3a95cdb02021-11-10T04:25:13ZActivation of the GLP-1 receptor by chloropyrimidine derivatives2211-715610.1016/j.rechem.2021.100222https://doaj.org/article/abf9bb2a2d3841919333302b3a95cdb02021-01-01T00:00:00Zhttp://www.sciencedirect.com/science/article/pii/S2211715621001272https://doaj.org/toc/2211-7156The anti-diabetic activities of a series of chloropyrimidine derviatives 2a-k and 4a-k were investigated after they were designed, synthesized, and docked against the GLP-1 receptor target. In comparison to exenatide, which was utilized as a reference drug, the three chloropyrimidine synthesized compounds 2c, 2f and 4c exhibited potent in vitro and in vivo antidiabetic activities. Interestingly, compounds 2c, 2f and 4c showed to be the most effective in lowering blood glucose levels and led to even higher glucose uptake than the reference drug, exenatide. Consistent with the in vitro and in vivo data, compounds 4c and 2f had the lowest docking energy scores (Glide-XP score = 5.1 kcal/mol) and the greatest ligand efficiency score (> − 0.40 kcal/mol) among all docked compounds. These findings give up new possibilities for the development of high-efficacy compounds to treat hyperglycemia.Shaikha S. AlNeyadiAbdu AdemNaheed AmerMohammad A GhattasNoor AtatrehAlaa A. SalemIbrahim M. AbdouElsevierarticleSynthesisType 2 diabetesGLP-1PyrimidineDockingChemistryQD1-999ENResults in Chemistry, Vol 3, Iss , Pp 100222- (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Synthesis Type 2 diabetes GLP-1 Pyrimidine Docking Chemistry QD1-999
spellingShingle	Synthesis Type 2 diabetes GLP-1 Pyrimidine Docking Chemistry QD1-999 Shaikha S. AlNeyadi Abdu Adem Naheed Amer Mohammad A Ghattas Noor Atatreh Alaa A. Salem Ibrahim M. Abdou Activation of the GLP-1 receptor by chloropyrimidine derivatives
description	The anti-diabetic activities of a series of chloropyrimidine derviatives 2a-k and 4a-k were investigated after they were designed, synthesized, and docked against the GLP-1 receptor target. In comparison to exenatide, which was utilized as a reference drug, the three chloropyrimidine synthesized compounds 2c, 2f and 4c exhibited potent in vitro and in vivo antidiabetic activities. Interestingly, compounds 2c, 2f and 4c showed to be the most effective in lowering blood glucose levels and led to even higher glucose uptake than the reference drug, exenatide. Consistent with the in vitro and in vivo data, compounds 4c and 2f had the lowest docking energy scores (Glide-XP score = 5.1 kcal/mol) and the greatest ligand efficiency score (> − 0.40 kcal/mol) among all docked compounds. These findings give up new possibilities for the development of high-efficacy compounds to treat hyperglycemia.
format	article
author	Shaikha S. AlNeyadi Abdu Adem Naheed Amer Mohammad A Ghattas Noor Atatreh Alaa A. Salem Ibrahim M. Abdou
author_facet	Shaikha S. AlNeyadi Abdu Adem Naheed Amer Mohammad A Ghattas Noor Atatreh Alaa A. Salem Ibrahim M. Abdou
author_sort	Shaikha S. AlNeyadi
title	Activation of the GLP-1 receptor by chloropyrimidine derivatives
title_short	Activation of the GLP-1 receptor by chloropyrimidine derivatives
title_full	Activation of the GLP-1 receptor by chloropyrimidine derivatives
title_fullStr	Activation of the GLP-1 receptor by chloropyrimidine derivatives
title_full_unstemmed	Activation of the GLP-1 receptor by chloropyrimidine derivatives
title_sort	activation of the glp-1 receptor by chloropyrimidine derivatives
publisher	Elsevier
publishDate	2021
url	https://doaj.org/article/abf9bb2a2d3841919333302b3a95cdb0
work_keys_str_mv	AT shaikhasalneyadi activationoftheglp1receptorbychloropyrimidinederivatives AT abduadem activationoftheglp1receptorbychloropyrimidinederivatives AT naheedamer activationoftheglp1receptorbychloropyrimidinederivatives AT mohammadaghattas activationoftheglp1receptorbychloropyrimidinederivatives AT nooratatreh activationoftheglp1receptorbychloropyrimidinederivatives AT alaaasalem activationoftheglp1receptorbychloropyrimidinederivatives AT ibrahimmabdou activationoftheglp1receptorbychloropyrimidinederivatives
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Activation of the GLP-1 receptor by chloropyrimidine derivatives

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