GPR109a agonists. Part 2: Pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109a

被引：10

作者：

Imbriglio, Jason E. ^{[1
]}

Chang, Sookhee ^{[1
]}

Liang, Rui ^{[1
]}

Raghavan, Subharekha ^{[1
]}

Schmidt, Darby ^{[1
]}

Smenton, Abby ^{[1
]}

Tria, Scott ^{[1
]}

Schrader, Thomas O. ^{[4
]}

Jung, Jae-Kyu ^{[4
]}

Esser, Craig ^{[1
]}

Holt, Tom G. ^{[2
]}

Wolff, Michael S. ^{[2
]}

Taggart, Andrew K. P. ^{[3
]}

Cheng, Kang ^{[3
]}

Carballo-Jane, Ester ^{[3
]}

Waters, M. Gerard ^{[3
]}

Tata, James R. ^{[1
]}

Colletti, Steven L. ^{[1
]}

机构：

[1] Merck & Co Inc, Dept Med Chem, Merck Res Labs, Rahway, NJ 07065 USA

[2] Merck & Co Inc, Dept Drug Metab, Merck Res Labs, Rahway, NJ 07065 USA

[3] Merck & Co Inc, Dept Cardiovasc Dis, Merck Res Labs, Rahway, NJ 07065 USA

[4] Arena Pharmaceut, Dept Med Chem, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 15期

关键词：

Niacin; GPR109a; Agonists; NICOTINIC-ACID; MOLECULAR-IDENTIFICATION;

D O I：

10.1016/j.bmcl.2010.06.041

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

5-Alkyl and aryl-pyrazole-acids have been identified as a new class of selective, small-molecule, agonists of the human orphan G-protein-coupled receptor GPR109a, a high affinity receptor for the HDL-raising drug nicotinic acid. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：4472 / 4474

页数：3

共 34 条

[1] GPR109a agonists. Part 1: 5-Alkyl and 5-aryl-pyrazole-tetrazoles as agonists of the human orphan G-protein coupled receptor GPR109a
Imbriglio, Jason E.
Chang, Sookhee
Liang, Rui
Raghavan, Subharekha
Schmidt, Darby
Smenton, Abby
Tria, Scott
Schrader, Thomas O.
Jung, Jae-Kyu
Esser, Craig
Taggart, Andrew K. P.
Cheng, Kang
Carballo-Jane, Ester
Waters, M. Gerard
Tata, James R.
Colletti, Steven L.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2009, 19 (08) : 2121 - 2124
[2] Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a
Skinner, Philip J.
Cherrier, Martin C.
Webb, Peter J.
Shin, Young-Jun
Gharbaoui, Tawfik
Lindstrom, Andrew
Hong, Vu
Tamura, Susan Y.
Dang, Huong T.
Pride, Cameron C.
Chen, Ruoping
Richman, Jeremy G.
Connolly, Daniel T.
Semple, Graeme
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (20) : 5620 - 5623
[3] Future of GPR109A agonists in the treatment of dyslipidaemia
Wanders, D.
Judd, R. L.
DIABETES OBESITY & METABOLISM, 2011, 13 (08) : 685 - 691
[4] Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a)
Boatman, P. Douglas
Schrader, Thomas O.
Kasem, Michelle
Johnson, Benjamin R.
Skinner, Philip J.
Jung, Jae-Kyu
Xu, Jerry
Cherrier, Martin C.
Webb, Peter J.
Semple, Graeme
Sage, Carleton R.
Knudsen, Jens
Chen, Ruoping
Taggart, Andrew K.
Carballo-Jane, Ester
Richman, Jeremy G.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2010, 20 (09) : 2797 - 2800
[5] High-Affinity Niacin Receptor GPR109A Agonists
Shen, Hong C.
Colletti, Steven L.
ANNUAL REPORTS IN MEDICINAL CHEMISTRY, VOL 45, 2010, 45 : 73 - +
[6] Discovery of novel pyrrole derivatives as potent agonists for the niacin receptor GPR109A
Miyazawa, Yuriko
Yamaguchi, Takahiro
Yamaguchi, Mitsuhiro
Tago, Keiko
Tamura, Akihiro
Sugiyama, Daisuke
Aburatani, Takahide
Nishizawa, Tomohiro
Kurikawa, Nobuya
Kono, Keita
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2020, 30 (10)
[7] The discovery of high affinity agonists of GPR109a with reduced serum shift and improved ADME properties
Imbriglio, Jason E.
DiRocco, Daniel
Bodner, Rena
Raghavan, Subharekha
Chen, Weichun
Marley, Daria
Esser, Craig
Holt, Tom G.
Wolff, Michael S.
Taggart, Andrew K. P.
Waters, M. Gerard
Tata, James R.
Colletti, Steven L.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2011, 21 (09) : 2721 - 2724
[8] Pyrido pyrimidinones as selective agonists of the high affinity niacin receptor GPR109A: Optimization of in vitro activity
Peters, Jens-Uwe
Kuehne, Holger
Dehmlow, Henrietta
Grether, Uwe
Conte, Aurelia
Hainzl, Dominik
Hertel, Cornelia
Kratochwil, Nicole A.
Otteneder, Michael
Narquizian, Robert
Panousis, Constantinos G.
Ricklin, Fabienne
Roever, Stephan
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2010, 20 (18) : 5426 - 5430
[9] Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109A
Ding, Fa-Xiang
Shen, Hong C.
Wilsie, Larrisa C.
Krsmanovic, Mihajlo L.
Taggart, Andrew K.
Ren, Ning
Cai, Tian-Quan
Wang, Junying
Tong, Xinchun
Holt, Tom G.
Chen, Qing
Waters, M. Gerard
Hammond, Milton L.
Tata, James R.
Colletti, Steven L.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2010, 20 (11) : 3372 - 3375
[10] Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109A
Shen, Hong C.
Szymonifka, Michael J.
Kharbanda, Divya
Denga, Qiaolin
Carballo-Jane, Ester
Wu, Kenneth K.
Wu, Tsuei-Ju
Cheng, Kang
Ren, Ning
Cai, Tian-Quan
Taggart, Andrew K.
Wang, Junying
Tong, Xinchun
Waters, M. Gerard
Hammond, Milton L.
Tata, James R.
Colletti, Steven L.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (24) : 6723 - 6728

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