Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)

Darren W Engers; Patrick R Gentry; Richard Williams; Julie D Bolinger; C David Weaver; Usha N Menon; P Jeffrey Conn; Craig W Lindsley; Colleen M Niswender; Corey R Hopkins

doi:10.1016/j.bmcl.2010.07.007

Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)

Darren W Engers, Patrick R Gentry, Richard Williams, Julie D Bolinger, C David Weaver, Usha N Menon, P Jeffrey Conn, Craig W Lindsley, Colleen M Niswender, Corey R Hopkins

21 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.

Original language	English
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	20
Issue number	17
Pages (from-to)	5175-8
Number of pages	4
ISSN	0960-894X
DOIs	https://doi.org/10.1016/j.bmcl.2010.07.007
Publication status	Published - 1 Sept 2010
Externally published	Yes

Keywords

Allosteric Regulation
Aniline Compounds/chemical synthesis
Receptors, Metabotropic Glutamate/drug effects
Structure-Activity Relationship
Sulfonamides/chemical synthesis

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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, U. N., Conn, P. J., Lindsley, C. W., Niswender, C. M., & Hopkins, C. R. (2010). Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS). Bioorganic & Medicinal Chemistry Letters, 20(17), 5175-8. https://doi.org/10.1016/j.bmcl.2010.07.007

Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS). / Engers, Darren W; Gentry, Patrick R; Williams, Richard et al.

In: Bioorganic & Medicinal Chemistry Letters, Vol. 20, No. 17, 01.09.2010, p. 5175-8.

Research output: Contribution to journal › Journal article › Research › peer-review

Engers, DW, Gentry, PR, Williams, R, Bolinger, JD, Weaver, CD, Menon, UN, Conn, PJ, Lindsley, CW, Niswender, CM & Hopkins, CR 2010, 'Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)', Bioorganic & Medicinal Chemistry Letters, vol. 20, no. 17, pp. 5175-8. https://doi.org/10.1016/j.bmcl.2010.07.007

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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.",

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AU - Gentry, Patrick R

AU - Williams, Richard

AU - Bolinger, Julie D

AU - Weaver, C David

AU - Menon, Usha N

AU - Conn, P Jeffrey

AU - Lindsley, Craig W

AU - Niswender, Colleen M

AU - Hopkins, Corey R

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KW - Allosteric Regulation

KW - Aniline Compounds/chemical synthesis

KW - Receptors, Metabotropic Glutamate/drug effects

KW - Structure-Activity Relationship

KW - Sulfonamides/chemical synthesis

U2 - 10.1016/j.bmcl.2010.07.007

DO - 10.1016/j.bmcl.2010.07.007

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JO - Bioorganic & Medicinal Chemistry Letters

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IS - 17

ER -

Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)

Abstract

Keywords

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