Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs)

Darren W. Engers; Colleen M. Niswender; C. David Weaver; Satyawan Jadhav; Usha N. Menon; Rocio Zamorano; P. Jeffrey Conn; Craig W. Lindsley; Corey R. Hopkins

doi:10.1021/jm9005065

Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs)

Darren W. Engers, Colleen M. Niswender, C. David Weaver, Satyawan Jadhav, Usha N. Menon, Rocio Zamorano, P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins

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

73 Scopus citations

Abstract

We report the synthesis and evaluation of a series of heterobiaryl amides as positive allosteric modulators of mGluR4. Compounds 9b and 9c showed submicromolar potency at both human and rat mGluR4. In addition, both 9b and 9c were shown to be centrally penetrant in rats using nontoxic vehicles, a major advance for the mGluR4 field.

Original language	English (US)
Pages (from-to)	4115-4118
Number of pages	4
Journal	Journal of Medicinal Chemistry
Volume	52
Issue number	14
DOIs	https://doi.org/10.1021/jm9005065
State	Published - Jul 23 2009
Externally published	Yes

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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Engers, D. W., Niswender, C. M., Weaver, C. D., Jadhav, S., Menon, U. N., Zamorano, R., Conn, P. J., Lindsley, C. W., & Hopkins, C. R. (2009). Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). Journal of Medicinal Chemistry, 52(14), 4115-4118. https://doi.org/10.1021/jm9005065

Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). / Engers, Darren W.; Niswender, Colleen M.; Weaver, C. David et al.
In: Journal of Medicinal Chemistry, Vol. 52, No. 14, 23.07.2009, p. 4115-4118.

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

Engers, DW, Niswender, CM, Weaver, CD, Jadhav, S, Menon, UN, Zamorano, R, Conn, PJ, Lindsley, CW & Hopkins, CR 2009, 'Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs)', Journal of Medicinal Chemistry, vol. 52, no. 14, pp. 4115-4118. https://doi.org/10.1021/jm9005065

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AU - Niswender, Colleen M.

AU - Weaver, C. David

AU - Jadhav, Satyawan

AU - Menon, Usha N.

AU - Zamorano, Rocio

AU - Conn, P. Jeffrey

AU - Lindsley, Craig W.

AU - Hopkins, Corey R.

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Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs)

Abstract

ASJC Scopus subject areas

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