N′,2-Diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists

Jason M. Elliott; Robert W. Carling; Mark Chambers; Gary G. Chicchi; Peter H. Hutson; A. Brian Jones; Angus MacLeod; Rose Marwood; Georgina Meneses-Lorente; Elena Mezzogori; Fraser Murray; Michael Rigby; Inmaculada Royo; Michael G N Russell; Bindi Sohal; Kwei Lan Tsao; Brian Williams

doi:10.1016/j.bmcl.2006.08.086

N′,2-Diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists

Jason M. Elliott
, Robert W. Carling
, Mark Chambers
, Gary G. Chicchi
, Peter H. Hutson
, A. Brian Jones
, Angus MacLeod
, Rose Marwood
, Georgina Meneses-Lorente
, Elena Mezzogori
, Fraser Murray
, Michael Rigby
, Inmaculada Royo
, Michael G N Russell
, Bindi Sohal
, Kwei Lan Tsao
, Brian Williams

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

Abstract

A new class of potent NK3R antagonists based on the N′,2-diphenylquinoline-4-carbohydrazide core is described. In an ex vivo assay in gerbil, the lead compound 2g occupies receptors within the CNS following oral dosing (Occ90 30 mg/kg po; plasma Occ90 0.95 μM) and has good selectivity and promising PK properties. © 2006 Elsevier Ltd. All rights reserved.

Original language	English
Pages (from-to)	5748-5751
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	16
Issue number	22
DOIs	https://doi.org/10.1016/j.bmcl.2006.08.086
Publication status	Published - 15 Nov 2006

Keywords

N′,2-Diphenylquinoline-4-carbohydrazide
NK3
Schizophrenia

Access to Document

10.1016/j.bmcl.2006.08.086

Cite this

Elliott, J. M., Carling, R. W., Chambers, M., Chicchi, G. G., Hutson, P. H., Jones, A. B., MacLeod, A., Marwood, R., Meneses-Lorente, G., Mezzogori, E., Murray, F., Rigby, M., Royo, I., Russell, M. G. N., Sohal, B., Tsao, K. L., & Williams, B. (2006). N′,2-Diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists. Bioorganic and Medicinal Chemistry Letters, 16(22), 5748-5751. https://doi.org/10.1016/j.bmcl.2006.08.086

@article{f386a332704143bf86eeeeb0f553dc53,

title = "N′,2-Diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists",

abstract = "A new class of potent NK3R antagonists based on the N′,2-diphenylquinoline-4-carbohydrazide core is described. In an ex vivo assay in gerbil, the lead compound 2g occupies receptors within the CNS following oral dosing (Occ90 30 mg/kg po; plasma Occ90 0.95 μM) and has good selectivity and promising PK properties. {\textcopyright} 2006 Elsevier Ltd. All rights reserved.",

keywords = "N′,2-Diphenylquinoline-4-carbohydrazide, NK3, Schizophrenia",

author = "Elliott, \{Jason M.\} and Carling, \{Robert W.\} and Mark Chambers and Chicchi, \{Gary G.\} and Hutson, \{Peter H.\} and Jones, \{A. Brian\} and Angus MacLeod and Rose Marwood and Georgina Meneses-Lorente and Elena Mezzogori and Fraser Murray and Michael Rigby and Inmaculada Royo and Russell, \{Michael G N\} and Bindi Sohal and Tsao, \{Kwei Lan\} and Brian Williams",

year = "2006",

month = nov,

day = "15",

doi = "10.1016/j.bmcl.2006.08.086",

language = "English",

volume = "16",

pages = "5748--5751",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "1464-3405",

publisher = "Elsevier BV",

number = "22",

}

Elliott, JM, Carling, RW, Chambers, M, Chicchi, GG, Hutson, PH, Jones, AB, MacLeod, A, Marwood, R, Meneses-Lorente, G, Mezzogori, E, Murray, F, Rigby, M, Royo, I, Russell, MGN, Sohal, B, Tsao, KL & Williams, B 2006, 'N′,2-Diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists', Bioorganic and Medicinal Chemistry Letters, vol. 16, no. 22, pp. 5748-5751. https://doi.org/10.1016/j.bmcl.2006.08.086

TY - JOUR

T1 - N′,2-Diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists

AU - Elliott, Jason M.

AU - Carling, Robert W.

AU - Chambers, Mark

AU - Chicchi, Gary G.

AU - Hutson, Peter H.

AU - Jones, A. Brian

AU - MacLeod, Angus

AU - Marwood, Rose

AU - Meneses-Lorente, Georgina

AU - Mezzogori, Elena

AU - Murray, Fraser

AU - Rigby, Michael

AU - Royo, Inmaculada

AU - Russell, Michael G N

AU - Sohal, Bindi

AU - Tsao, Kwei Lan

AU - Williams, Brian

PY - 2006/11/15

Y1 - 2006/11/15

N2 - A new class of potent NK3R antagonists based on the N′,2-diphenylquinoline-4-carbohydrazide core is described. In an ex vivo assay in gerbil, the lead compound 2g occupies receptors within the CNS following oral dosing (Occ90 30 mg/kg po; plasma Occ90 0.95 μM) and has good selectivity and promising PK properties. © 2006 Elsevier Ltd. All rights reserved.

AB - A new class of potent NK3R antagonists based on the N′,2-diphenylquinoline-4-carbohydrazide core is described. In an ex vivo assay in gerbil, the lead compound 2g occupies receptors within the CNS following oral dosing (Occ90 30 mg/kg po; plasma Occ90 0.95 μM) and has good selectivity and promising PK properties. © 2006 Elsevier Ltd. All rights reserved.

KW - N′,2-Diphenylquinoline-4-carbohydrazide

KW - NK3

KW - Schizophrenia

U2 - 10.1016/j.bmcl.2006.08.086

DO - 10.1016/j.bmcl.2006.08.086

M3 - Article

C2 - 16950620

SN - 1464-3405

VL - 16

SP - 5748

EP - 5751

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 22

ER -

N′,2-Diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists

Abstract

Keywords

Access to Document

Fingerprint

Cite this