Novel substituted 4-aminomethylpiperidines as potent and selective human β3-agonists.: Part 2:: Arylethanolaminomethylpiperidines

被引:7
|
作者
Steffan, RJ
Ashwell, MA
Solvibile, WR
Matelan, E
Largis, E
Han, S
Tillet, J
Mulvey, R
机构
[1] Wyeth Ayerst Res, Chem Sci, Collegeville, PA 19426 USA
[2] Wyeth Ayerst Res, Cardiovasc Metab Dis, Collegeville, PA 19426 USA
关键词
D O I
10.1016/S0960-894X(02)00608-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis and SAR of a series of beta(3) adrenoreceptor agonists based on a novel template derived from 4-aminomethylpiperidine coupled with a common pharmacophore, arylethylamine, is described. This combination led to the identification of human beta(3) adrenoreceptor agonists with in vivo activity in a transgenic mouse model. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2963 / 2967
页数:5
相关论文
共 50 条
  • [1] Novel substituted 4-aminomethylpiperidines as potent and selective human β3-agonists.: Part 1:: Aryloxypropanolaminomethylpiperidines
    Steffan, RJ
    Ashwell, MA
    Solvibile, WR
    Matelan, E
    Largis, E
    Han, S
    Tillet, J
    Mulvey, R
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2002, 12 (20) : 2957 - 2961
  • [2] 4-Substituted piperidines:: Potent, selective agonists of the human β3-adrenergic receptor.
    Ashwell, MA
    Solvibile, WR
    [J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2001, 221 : U41 - U41
  • [3] SAR development of novel substituted 2-(S)-hydroxy-3-(piperidin-4-yl-methylamino)-propyl ethers and substituted 2-aryl-2-(R)-hydroxy-1-(piperidin-4-yl-methyl)-ethylamine compounds as potent and selective human β3-agonists.
    Steffan, RJ
    Ashwell, MA
    Solvibile, WR
    Matelan, E
    [J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2001, 221 : U41 - U41
  • [4] Novel (4-piperidin-1-yl)-phenyl sulfonamides as potent and selective human β3 agonists
    Hu, BH
    Ellingboe, J
    Han, S
    Largis, E
    Lim, K
    Malamas, M
    Mulvey, R
    Niu, CS
    Oliphant, A
    Pelletier, J
    Singanallore, T
    Sum, FW
    Tillett, J
    Wong, V
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY, 2001, 9 (08) : 2045 - 2059
  • [5] 2,4-thiazolidinediones as potent and selective human β3 agonists
    Hu, BH
    Ellingboe, J
    Gunawan, I
    Han, S
    Largis, E
    Li, ZA
    Malamas, M
    Mulvey, R
    Oliphant, A
    Sum, FW
    Tillett, J
    Wong, V
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (06) : 757 - 760
  • [6] New substituted MECA derivatives as potent and selective agonists for the human adenosine A3 receptor
    Lambertucci, Catia
    Dal Ben, Diego
    Lammi, Carmen
    Marucci, Gabriella
    Ramadori, Anna Teresa
    Volpini, Rosaria
    Klotz, Karl-Norbert
    Cristalli, Gloria
    [J]. PURINERGIC SIGNALLING, 2010, 6 (01) : 91 - 91
  • [7] 2 NOVEL, POTENT AND SELECTIVE HISTAMINE H-3 RECEPTOR AGONISTS
    HOWSON, W
    PARSONS, ME
    RAVAL, P
    SWAYNE, GTG
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1992, 2 (01) : 77 - 78
  • [8] Potent, selective aminothiazolidinediones agonists of the human β3 adrenergic receptor
    Malamas, MS
    Largis, E
    Gunawan, I
    Li, ZN
    Tillett, J
    Han, SCH
    Mulvey, R
    [J]. MEDICINAL CHEMISTRY RESEARCH, 2000, 10 (03) : 164 - 177
  • [9] Potent, selective benzenesulfonamide agonists of the human β3 adrenergic receptor
    Weber, AE
    Mathvink, RJ
    Perkins, L
    Hutchins, JE
    Candelore, MR
    Tota, L
    Strader, CD
    Wyvratt, MJ
    Fisher, MH
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (09) : 1101 - 1106
  • [10] New oxadiazolidinedione derivatives as potent and selective human β3 agonists
    Hu, BH
    Malamas, M
    Ellingboe, J
    Largis, E
    Han, S
    Mulvey, R
    Tillett, J
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (08) : 981 - 984