3-Nitro-4-amino benzoic acids and 6-amino nicotinic acids are highly selective agonists of GPR109b

被引：22

作者：

Skinner, Philip J. ^{[1
]}

Cherrier, Martin C. ^{[1
]}

Webb, Peter J. ^{[1
]}

Sage, Carleton R. ^{[1
]}

Dang, Huong T. ^{[1
]}

Pride, Cameron C. ^{[1
]}

Chen, Ruoping ^{[1
]}

Tamura, Susan Y. ^{[1
]}

Richman, Jeremy G. ^{[1
]}

Connolly, Daniel T. ^{[1
]}

Semple, Graeme ^{[1
]}

机构：

[1] Arena Pharmaceut, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 23期

关键词：

D O I：

10.1016/j.bmcl.2007.09.058

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 3-nitro-4-substituted-aminobenzoic acids were prepared and found to act as potent and highly selective agonists of the orphan human GPCR GPR109b, a low affinity receptor for niacin. No activity was observed at the closely homologous high affinity niacin receptor, GPR109a. A second series, comprising 6-amino-substituted nicotinic acids was, also prepared and several analogues showed comparable activity to the nitroaryl series. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：6619 / 6622

页数：4

共 50 条

[31] Diastereoselective synthesis of highly functionalized β2,2,3-substituted amino acids from 4-substituted-1,3-oxazinan-6-ones
Nguyen, Nghi H.
Sleebs, Brad E.
White, Jonathan M.
Hughes, Andrew B.
TETRAHEDRON, 2012, 68 (24) : 4745 - 4756
[32] Simple, Highly Enantioselective Access to Quaternary 1,3,4,4-Tetrasubstituted β-Lactams from Amino Acids: A Solid-Phase Approach
Perez-Faginas, Paula
Aranda, M. Teresa
Coady, Laoise
Garcia-Lopez, M. Teresa
Gonzalez-Muniz, Rosario
ADVANCED SYNTHESIS & CATALYSIS, 2008, 350 (14-15) : 2279 - 2285
[33] Age-dependent alteration in metabolism of vitamin B-6, neurotransmitters, and amino acids after 4 '-O-methylpyridoxine administration in rats
Zhu, Jin-Peng
Gong, Hao
Labreche, Faiza
Kou, Xiao-Hong
Wu, Cai-E
Fan, Gong-Jian
Li, Ting-Ting
Wang, Jia-Hong
Shen, Dong-Bei
JOURNAL OF FOOD SCIENCE, 2022, 87 (01) : 466 - 480
[34] Synthesis and performance of 7-amino-6-nitro-[1, 2, 5]oxadiazolo[3, 4-b]pyridine-1-oxide
Ma, Cong-Ming
Wang, Yong-Bin
Liu, Zu-Liang
Yao, Qi-Zheng
Hanneng Cailiao/Chinese Journal of Energetic Materials, 2014, 22 (04): : 572 - 575
[35] SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF 2-AMINO-5-ARYL-5H-THIAZOLO [4,3-b]-1,3,4-THIADIAZOLE DERIVATIVES OF AMINO ACIDS AND PEPTIDES
Himaja, M.
Karigar, Asif A.
Prathap, Jagadeesh K.
Ramana, M. V.
Mali, Sunil V.
INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY, 2011, 21 (02) : 125 - 128
[36] AMIDES OF N-[3-NITRO(AMINO)COUMARIN-4-YL]ANTHRANYLIC ACIDS - SYNTHESIS OF 6,7,8,13-TETRAHYDRO[1]BENZOPYRANO[4,3-B][1,4]BENZODIAZEPINE-6,8-DIONE
SAVELEV, VL
ARTAMONOVA, OS
MAKAROV, AV
TROITSKAYA, VS
ANTONOVA, AV
VINOKUROV, VG
KHIMIYA GETEROTSIKLICHESKIKH SOEDINENII, 1989, (09): : 1208 - 1212
[37] Identification of 4-(6-((2-methoxyphenyl)amino)pyrazin-2-yl)benzoic acids as CSNK2A inhibitors with antiviral activity and improved selectivity over PIM3
Galal, Kareem A.
Kraemer, Andreas
Strickland, Benjamin G.
Smith, Jeffery L.
Dickmander, Rebekah J.
Moorman, Nathaniel J.
Willson, Timothy M.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2024, 99
[38] 1H and 13C NMR determination of the enantiomeric purity of substituted 4-amino-3-(thien-2-yl)-butyric acids and 4-amino-3-(benzo[b]furan-2-yl)-butyric acids, ligands of the GABAB receptor.
Al Akoum-Ebrik, S
Ansar, M
Mouhoub, R
Vaccher, C
Vaccher, MP
Flouquet, N
SPECTROSCOPY LETTERS, 1998, 31 (05) : 925 - 944
[39] POTENTIAL FOLIC ACID ANTAGONISTS .4. SYNTHETIC APPROACHES TO ANALOGS OF AMINOPTERIN AND METHOTREXATE .4. PREPARATION OF PARA-([(2,4-DIAMINO-6-PTERIDINYL)METHYL]AMINO)-BENZOIC ACIDS
ELLIOTT, RD
TEMPLE, C
MONTGOMERY, JA
JOURNAL OF ORGANIC CHEMISTRY, 1970, 35 (05): : 1676 - +
[40] CHAIN ELONGATION OF AROMATIC AMINO-ACIDS - ROLE OF 2-BENZYLMALIC ACID IN BIOSYNTHESIS OF A C6C4 AMINO-ACID AND A C6C3 MUSTARD OIL GLUCOSIDE
DORNEMANN, D
LOFFELHARDT, W
KINDL, H
CANADIAN JOURNAL OF BIOCHEMISTRY, 1974, 52 (10): : 916 - 921

← 1 2 3 4 5 →