Polar aromatic periphery increases agonist potency of spirocyclic free fatty acid receptor (GPR40) agonists inspired by LY2881835
Mikhail Krasavin
1
,
Alexey Lukin
2
,
Daria Bagnyukova
2
,
Nikolay Zhurilo
2
,
Sergey Zozulya
3, 4
,
Ihor Zahanich#
5
,
Daniel S Moore
6
,
Irina A. Tikhonova
6
3
Enamine Ltd, 78 Chervonotkatska, Kyiv 02094, Ukraine
|
4
Taras Shevchenko National University, 62 Volodymyrska, Kyiv 01033, Ukraine.
|
5
Enamine Ltd, 78 Chervonotkatska, Kyiv 02094, Ukraine.
|
Publication type: Journal Article
Publication date: 2017-02-01
scimago Q1
wos Q1
SJR: 1.142
CiteScore: 11.3
Impact factor: 5.9
ISSN: 02235234, 17683254
PubMed ID:
28076825
Organic Chemistry
Drug Discovery
General Medicine
Pharmacology
Abstract
A series of spirocyclic compounds inspired by Eli Lilly's phase 1 antidiabetic FFA1 receptor agonist LY2881835 was designed to include polar aromatic periphery groups and explore a possibility of building additional contacts with the target near the agonist binding site. The frontrunner compound in the series (9i) was shown to be a potent (EC50 = 260 nM) FFA1 agonist with excellent aqueous (PBS) solubility and good Caco-2 permeability. The observed structure-activity relationships were rationalized by a docking study. The new series significantly expands the ligand landscape for the ongoing quest for new potent and more polar FFA1 agonists as fundamentally new class of therapeutic agents against type 2 diabetes mellitus.
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Total citations:
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Citations from 2025:
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Krasavin M. et al. Polar aromatic periphery increases agonist potency of spirocyclic free fatty acid receptor (GPR40) agonists inspired by LY2881835 // European Journal of Medicinal Chemistry. 2017. Vol. 127. pp. 357-368.
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Krasavin M., Lukin A., Bagnyukova D., Zhurilo N., Golovanov A., Zozulya S., Zahanich# I., Moore D. S., Tikhonova I. A. Polar aromatic periphery increases agonist potency of spirocyclic free fatty acid receptor (GPR40) agonists inspired by LY2881835 // European Journal of Medicinal Chemistry. 2017. Vol. 127. pp. 357-368.
Cite this
RIS
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TY - JOUR
DO - 10.1016/j.ejmech.2017.01.005
UR - https://doi.org/10.1016/j.ejmech.2017.01.005
TI - Polar aromatic periphery increases agonist potency of spirocyclic free fatty acid receptor (GPR40) agonists inspired by LY2881835
T2 - European Journal of Medicinal Chemistry
AU - Krasavin, Mikhail
AU - Lukin, Alexey
AU - Bagnyukova, Daria
AU - Zhurilo, Nikolay
AU - Golovanov, Aleksei
AU - Zozulya, Sergey
AU - Zahanich#, Ihor
AU - Moore, Daniel S
AU - Tikhonova, Irina A.
PY - 2017
DA - 2017/02/01
PB - Elsevier
SP - 357-368
VL - 127
PMID - 28076825
SN - 0223-5234
SN - 1768-3254
ER -
Cite this
BibTex (up to 50 authors)
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@article{2017_Krasavin,
author = {Mikhail Krasavin and Alexey Lukin and Daria Bagnyukova and Nikolay Zhurilo and Aleksei Golovanov and Sergey Zozulya and Ihor Zahanich# and Daniel S Moore and Irina A. Tikhonova},
title = {Polar aromatic periphery increases agonist potency of spirocyclic free fatty acid receptor (GPR40) agonists inspired by LY2881835},
journal = {European Journal of Medicinal Chemistry},
year = {2017},
volume = {127},
publisher = {Elsevier},
month = {feb},
url = {https://doi.org/10.1016/j.ejmech.2017.01.005},
pages = {357--368},
doi = {10.1016/j.ejmech.2017.01.005}
}
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