Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS

A.L. Rodriguez; Y. Zhou; Richard Williams; C.D. Weaver; P.J. Conn; C.W. Lindsley

doi:10.1016/j.bmcl.2009.10.059

Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS

A.L. Rodriguez
, Y. Zhou
, Richard Williams
, C.D. Weaver
, P.J. Conn
, C.W. Lindsley

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

19 Citations (Scopus)

Abstract

This Letter describes the discovery and SAR of three novel series of mGluR5 non-competitive antagonists/negative allosteric modulators (NAMs) not based on manipulation of an MPEP/MTEP chemotype identified by a functional HTS approach. This work demonstrates fundamentally new mGluR5 NAM chemotypes with submicromolar potencies, and further examples of a mode of pharmacology 'switch' to provide PAMs with a non-MPEP scaffold. (C) 2009 Elsevier Ltd. All rights reserved.

Original language	English
Pages (from-to)	6502-6506
Number of pages	5
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	19
Issue number	23
DOIs	https://doi.org/10.1016/j.bmcl.2009.10.059
Publication status	Published - 01 Dec 2009

ASJC Scopus subject areas

Pharmaceutical Science
Drug Discovery
Organic Chemistry
Molecular Medicine
Molecular Biology
Clinical Biochemistry
Biochemistry

Access to Document

10.1016/j.bmcl.2009.10.059

Cite this

@article{3cab5239032c42bca4588cffb14eb0fc,

title = "Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS",

abstract = "This Letter describes the discovery and SAR of three novel series of mGluR5 non-competitive antagonists/negative allosteric modulators (NAMs) not based on manipulation of an MPEP/MTEP chemotype identified by a functional HTS approach. This work demonstrates fundamentally new mGluR5 NAM chemotypes with submicromolar potencies, and further examples of a mode of pharmacology 'switch' to provide PAMs with a non-MPEP scaffold. (C) 2009 Elsevier Ltd. All rights reserved.",

author = "A.L. Rodriguez and Y. Zhou and Richard Williams and C.D. Weaver and P.J. Conn and C.W. Lindsley",

year = "2009",

month = dec,

day = "1",

doi = "10.1016/j.bmcl.2009.10.059",

language = "English",

volume = "19",

pages = "6502--6506",

journal = "Bioorganic \& Medicinal Chemistry Letters",

issn = "1464-3405",

publisher = "Elsevier Ltd",

number = "23",

}

TY - JOUR

T1 - Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS

AU - Rodriguez, A.L.

AU - Zhou, Y.

AU - Williams, Richard

AU - Weaver, C.D.

AU - Conn, P.J.

AU - Lindsley, C.W.

PY - 2009/12/1

Y1 - 2009/12/1

N2 - This Letter describes the discovery and SAR of three novel series of mGluR5 non-competitive antagonists/negative allosteric modulators (NAMs) not based on manipulation of an MPEP/MTEP chemotype identified by a functional HTS approach. This work demonstrates fundamentally new mGluR5 NAM chemotypes with submicromolar potencies, and further examples of a mode of pharmacology 'switch' to provide PAMs with a non-MPEP scaffold. (C) 2009 Elsevier Ltd. All rights reserved.

AB - This Letter describes the discovery and SAR of three novel series of mGluR5 non-competitive antagonists/negative allosteric modulators (NAMs) not based on manipulation of an MPEP/MTEP chemotype identified by a functional HTS approach. This work demonstrates fundamentally new mGluR5 NAM chemotypes with submicromolar potencies, and further examples of a mode of pharmacology 'switch' to provide PAMs with a non-MPEP scaffold. (C) 2009 Elsevier Ltd. All rights reserved.

U2 - 10.1016/j.bmcl.2009.10.059

DO - 10.1016/j.bmcl.2009.10.059

M3 - Article

SN - 1464-3405

VL - 19

SP - 6502

EP - 6506

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 23

ER -

Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS

Abstract

ASJC Scopus subject areas

Access to Document

Fingerprint

Cite this