Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists

Jason Witherington; Vincent Bordas; Dave G. Cooper; Ian T. Forbes; Andrew D. Gribble; Robert J. Ife; Theo Berkhout; Jayneeta Gohil; Pieter H. E. Groot

doi:10.1016/S0960-894X(01)00397-3

Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists

Jason Witherington, Vincent Bordas, Dave G. Cooper, Ian T. Forbes, Andrew D. Gribble, Robert J. Ife, Theo Berkhout, Jayneeta Gohil, Pieter H. E. Groot

School of Life and Medical Sciences

Research output: Contribution to journal › Article › peer-review

47 Citations (Scopus)

Abstract

The preparation and biological evaluation of a series of indolopiperidine CCR2B receptor antagonists possessing a conformationally restricted C-5 linker chain in combination with a restricted piperidine ring are described. Compared to the parent compound 1, analogue 8 shows a dramatic improvement in selectivity against a range of 5-HT and dopaminergic receptors.

Original language	English
Pages (from-to)	2177-2180
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	11
Issue number	16
DOIs	https://doi.org/10.1016/S0960-894X(01)00397-3
Publication status	Published - 20 Aug 2001

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title = "Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists",

abstract = "The preparation and biological evaluation of a series of indolopiperidine CCR2B receptor antagonists possessing a conformationally restricted C-5 linker chain in combination with a restricted piperidine ring are described. Compared to the parent compound 1, analogue 8 shows a dramatic improvement in selectivity against a range of 5-HT and dopaminergic receptors.",

author = "Jason Witherington and Vincent Bordas and Cooper, \{Dave G.\} and Forbes, \{Ian T.\} and Gribble, \{Andrew D.\} and Ife, \{Robert J.\} and Theo Berkhout and Jayneeta Gohil and Groot, \{Pieter H. E.\}",

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T1 - Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists

AU - Witherington, Jason

AU - Bordas, Vincent

AU - Cooper, Dave G.

AU - Forbes, Ian T.

AU - Gribble, Andrew D.

AU - Ife, Robert J.

AU - Berkhout, Theo

AU - Gohil, Jayneeta

AU - Groot, Pieter H. E.

PY - 2001/8/20

Y1 - 2001/8/20

N2 - The preparation and biological evaluation of a series of indolopiperidine CCR2B receptor antagonists possessing a conformationally restricted C-5 linker chain in combination with a restricted piperidine ring are described. Compared to the parent compound 1, analogue 8 shows a dramatic improvement in selectivity against a range of 5-HT and dopaminergic receptors.

AB - The preparation and biological evaluation of a series of indolopiperidine CCR2B receptor antagonists possessing a conformationally restricted C-5 linker chain in combination with a restricted piperidine ring are described. Compared to the parent compound 1, analogue 8 shows a dramatic improvement in selectivity against a range of 5-HT and dopaminergic receptors.

U2 - 10.1016/S0960-894X(01)00397-3

DO - 10.1016/S0960-894X(01)00397-3

M3 - Article

C2 - 11514164

AN - SCOPUS:0035921020

SN - 0960-894X

VL - 11

SP - 2177

EP - 2180

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 16

ER -

Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists

Abstract

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