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 Citationer (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.

Originalsprog	Engelsk
Tidsskrift	Bioorganic & Medicinal Chemistry Letters
Vol/bind	20
Udgave nummer	17
Sider (fra-til)	5175-8
Antal sider	4
ISSN	0960-894X
DOI	https://doi.org/10.1016/j.bmcl.2010.07.007
Status	Udgivet - 1 sep. 2010
Udgivet eksternt	Ja

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10.1016/j.bmcl.2010.07.007

Citationsformater

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.
I: Bioorganic & Medicinal Chemistry Letters, Bind 20, Nr. 17, 01.09.2010, s. 5175-8.

Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › 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, bind 20, nr. 17, s. 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 - 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

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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

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