Standard
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; Bolinger, Julie D; Weaver, C David; Menon, Usha N; Conn, P Jeffrey; Lindsley, Craig W; Niswender, Colleen M; Hopkins, Corey R.
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
Harvard
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.2010.07.007APA
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.2010.07.007Vancouver
Engers DW, Gentry PR, Williams R, Bolinger JD, Weaver CD, Menon UN et al.
Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS).
Bioorganic & Medicinal Chemistry Letters. 2010 Sep 1;20(17):5175-8.
https://doi.org/10.1016/j.bmcl.2010.07.007Author
Engers, Darren W ; Gentry, Patrick R ; Williams, Richard ; Bolinger, Julie D ; Weaver, C David ; Menon, Usha N ; Conn, P Jeffrey ; Lindsley, Craig W ; Niswender, Colleen M ; Hopkins, Corey R. / Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS). In: Bioorganic & Medicinal Chemistry Letters. 2010 ; Vol. 20, No. 17. pp. 5175-8.
Bibtex
@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}",
note = "Copyright 2010 Elsevier Ltd. All rights reserved.",
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",
}
RIS
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
N1 - Copyright 2010 Elsevier Ltd. All rights reserved.
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
VL - 20
SP - 5175
EP - 5178
JO - Bioorganic & Medicinal Chemistry Letters
JF - Bioorganic & Medicinal Chemistry Letters
SN - 0960-894X
IS - 17
ER -
