A New Pyridazine Series of GABAA α5 Ligands

M.B. Van Niel; K. Wilson; C.H. Adkins; J.R. Atack; J.L. Castro; D.E. Clarke; S. Fletcher; U. Gerhard; M.M. Mackey; S. Malpas; K. Maubach; R. Newman; D. O'Connor; G.V. Pillai; P.B. Simpson; S.R. Thomas; A.M. MacLeod

doi:10.1021/jm050249x

A New Pyridazine Series of GABA_A α5 Ligands

M.B. Van Niel, K. Wilson, C.H. Adkins, J.R. Atack, J.L. Castro, D.E. Clarke, S. Fletcher, U. Gerhard, M.M. Mackey, S. Malpas, K. Maubach, R. Newman, D. O'Connor, G.V. Pillai, P.B. Simpson, S.R. Thomas, A.M. MacLeod

School of Life and Medical Sciences

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

16 Citations (Scopus)

Abstract

Screening of the Merck compound collection identified 6 as an unusually simple, low molecular weight hit with moderate affinity for GABA_A receptors. The structural novelty of 6, compared to our advanced series of GABA_A α5 inverse agonists, made it an attractive molecule for further exploration. This paper will describe the evolution of 6 into a new series of ligands with nanomolar affinity and functional selectivity for GABA_Aα5 receptor subtypes.

Original language	English
Pages (from-to)	6004-6011
Number of pages	8
Journal	Journal of Medicinal Chemistry
Volume	48
Issue number	19
DOIs	https://doi.org/10.1021/jm050249x
Publication status	Published - 22 Sept 2005

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Van Niel, M. B., Wilson, K., Adkins, C. H., Atack, J. R., Castro, J. L., Clarke, D. E., Fletcher, S., Gerhard, U., Mackey, M. M., Malpas, S., Maubach, K., Newman, R., O'Connor, D., Pillai, G. V., Simpson, P. B., Thomas, S. R., & MacLeod, A. M. (2005). A New Pyridazine Series of GABA_A α5 Ligands. Journal of Medicinal Chemistry, 48(19), 6004-6011. https://doi.org/10.1021/jm050249x

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abstract = "Screening of the Merck compound collection identified 6 as an unusually simple, low molecular weight hit with moderate affinity for GABAA receptors. The structural novelty of 6, compared to our advanced series of GABAA α5 inverse agonists, made it an attractive molecule for further exploration. This paper will describe the evolution of 6 into a new series of ligands with nanomolar affinity and functional selectivity for GABAA α5 receptor subtypes.",

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AU - Van Niel, M.B.

AU - Wilson, K.

AU - Adkins, C.H.

AU - Atack, J.R.

AU - Castro, J.L.

AU - Clarke, D.E.

AU - Fletcher, S.

AU - Gerhard, U.

AU - Mackey, M.M.

AU - Malpas, S.

AU - Maubach, K.

AU - Newman, R.

AU - O'Connor, D.

AU - Pillai, G.V.

AU - Simpson, P.B.

AU - Thomas, S.R.

AU - MacLeod, A.M.

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AB - Screening of the Merck compound collection identified 6 as an unusually simple, low molecular weight hit with moderate affinity for GABAA receptors. The structural novelty of 6, compared to our advanced series of GABAA α5 inverse agonists, made it an attractive molecule for further exploration. This paper will describe the evolution of 6 into a new series of ligands with nanomolar affinity and functional selectivity for GABAA α5 receptor subtypes.

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A New Pyridazine Series of GABA_A α5 Ligands

Abstract

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