Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu(4) positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)

D.W. Engers; P.R. Gentry; Richard Williams; J.D. Bolinger; C.D. Weaver; Aric Menon; Lorna Conn; C.W. Lindsley; C.M. Niswender; Fiona Hopkins

doi:10.1016/j.bmcl.2010.07.007

Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu(4) positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)

D.W. Engers
, P.R. Gentry
, Richard Williams
, J.D. Bolinger
, C.D. Weaver
, Aric Menon
, Lorna Conn
, C.W. Lindsley
, C.M. Niswender
, Fiona Hopkins

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

25 Citations (Scopus)

Abstract

Herein we disclose the synthesis and SAR of a series of 4-(phenylsulfamoyl)phenylacetamide compounds as mGlu(4) positive allosteric modulators (PAMs) that were identified via a functional HTS. An iterative parallel approach to these compounds culminated in the discovery of VU0364439 (11) which represents the most potent (19.8 nM) mGlu(4) PAM reported to date. (C) 2010 Elsevier Ltd. All rights reserved.

Original language	English
Pages (from-to)	5175-5178
Number of pages	4
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	20
Issue number	17
DOIs	https://doi.org/10.1016/j.bmcl.2010.07.007
Publication status	Published - 01 Sept 2010

ASJC Scopus subject areas

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

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10.1016/j.bmcl.2010.07.007

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Engers, D. W., Gentry, P. R., Williams, R., Bolinger, J. D., Weaver, C. D., Menon, A., Conn, L., Lindsley, C. W., Niswender, C. M., & Hopkins, F. (2010). Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu(4) positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS). Bioorganic & Medicinal Chemistry Letters, 20(17), 5175-5178. https://doi.org/10.1016/j.bmcl.2010.07.007

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title = "Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu(4) positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)",

abstract = "Herein we disclose the synthesis and SAR of a series of 4-(phenylsulfamoyl)phenylacetamide compounds as mGlu(4) positive allosteric modulators (PAMs) that were identified via a functional HTS. An iterative parallel approach to these compounds culminated in the discovery of VU0364439 (11) which represents the most potent (19.8 nM) mGlu(4) PAM reported to date. (C) 2010 Elsevier Ltd. All rights reserved.",

author = "D.W. Engers and P.R. Gentry and Richard Williams and J.D. Bolinger and C.D. Weaver and Aric Menon and Lorna Conn and C.W. Lindsley and C.M. Niswender and Fiona Hopkins",

year = "2010",

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doi = "10.1016/j.bmcl.2010.07.007",

language = "English",

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Engers, DW, Gentry, PR, Williams, R, Bolinger, JD, Weaver, CD, Menon, A, Conn, L, Lindsley, CW, Niswender, CM & Hopkins, F 2010, 'Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu(4) positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)', Bioorganic & Medicinal Chemistry Letters, vol. 20, no. 17, pp. 5175-5178. https://doi.org/10.1016/j.bmcl.2010.07.007

Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu(4) positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS). / Engers, D.W.; Gentry, P.R.; Williams, Richard et al.
In: Bioorganic & Medicinal Chemistry Letters, Vol. 20, No. 17, 01.09.2010, p. 5175-5178.

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

TY - JOUR

T1 - Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu(4) positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)

AU - Engers, D.W.

AU - Gentry, P.R.

AU - Williams, Richard

AU - Bolinger, J.D.

AU - Weaver, C.D.

AU - Menon, Aric

AU - Conn, Lorna

AU - Lindsley, C.W.

AU - Niswender, C.M.

AU - Hopkins, Fiona

PY - 2010/9/1

Y1 - 2010/9/1

N2 - Herein we disclose the synthesis and SAR of a series of 4-(phenylsulfamoyl)phenylacetamide compounds as mGlu(4) positive allosteric modulators (PAMs) that were identified via a functional HTS. An iterative parallel approach to these compounds culminated in the discovery of VU0364439 (11) which represents the most potent (19.8 nM) mGlu(4) PAM reported to date. (C) 2010 Elsevier Ltd. All rights reserved.

AB - Herein we disclose the synthesis and SAR of a series of 4-(phenylsulfamoyl)phenylacetamide compounds as mGlu(4) positive allosteric modulators (PAMs) that were identified via a functional HTS. An iterative parallel approach to these compounds culminated in the discovery of VU0364439 (11) which represents the most potent (19.8 nM) mGlu(4) PAM reported to date. (C) 2010 Elsevier Ltd. All rights reserved.

U2 - 10.1016/j.bmcl.2010.07.007

DO - 10.1016/j.bmcl.2010.07.007

M3 - Article

SN - 1464-3405

VL - 20

SP - 5175

EP - 5178

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 17

ER -

Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu(4) positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)

Abstract

ASJC Scopus subject areas

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