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

Access to Document

10.1016/j.bmcl.2010.07.007

Cite this

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

@article{fef36a22be6f4ed18d09a8c3ee27367c,

title = "Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 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.",

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

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

year = "2010",

month = sep,

day = "1",

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

language = "English",

volume = "20",

pages = "5175--8",

journal = "Bioorganic & Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Pergamon Press",

number = "17",

}

TY - JOUR

T1 - Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)

AU - Engers, Darren W

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

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.

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.

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

M3 - Journal article

C2 - 20667732

SN - 0960-894X

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 mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)

Abstract

Keywords

Access to Document

Fingerprint

Cite this