Potent antagonists of gonadotropin releasing hormone receptors derived from quinolone-6-carboxamides

Thomas F. Walsh; Richard B. Toupence; Jonathan R. Young; Song X. Huang; Feroze Ujjainwalla; Robert J. Devita; Mark T. Goulet; Matthew J. Wyvratt; Michael H. Fisher; Jane Ling Lo; Ning Ren; Joel B. Yudkovitz; Yi Tien Yang; Kang Cheng; Roy G. Smith

doi:10.1016/S0960-894X(00)00024-X

Potent antagonists of gonadotropin releasing hormone receptors derived from quinolone-6-carboxamides

Thomas F. Walsh, Richard B. Toupence, Jonathan R. Young, Song X. Huang, Feroze Ujjainwalla, Robert J. Devita, Mark T. Goulet, Matthew J. Wyvratt, Michael H. Fisher, Jane Ling Lo, Ning Ren, Joel B. Yudkovitz, Yi Tien Yang, Kang Cheng, Roy G. Smith

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51 Scopus citations

Abstract

SAR studies which focused upon the C-6 position of a recently described series of quinolone gonadotropin releasing hormone antagonists are reported. Synthetic access to diverse quinolone-6-carboxamides was achieved via the palladium-catalyzed amino-carbonylation reactions of iodide 4 with various amines. Amides related to 9y were especially potent, functional antagonists of rat and human GnRH receptors. (C) 2000 Elsevier Science Ltd. All rights reserved.

Original language	English
Pages (from-to)	443-447
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	10
Issue number	5
DOIs	https://doi.org/10.1016/S0960-894X(00)00024-X
State	Published - 6 Mar 2000
Externally published	Yes

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Walsh, T. F., Toupence, R. B., Young, J. R., Huang, S. X., Ujjainwalla, F., Devita, R. J., Goulet, M. T., Wyvratt, M. J., Fisher, M. H., Lo, J. L., Ren, N., Yudkovitz, J. B., Yang, Y. T., Cheng, K., & Smith, R. G. (2000). Potent antagonists of gonadotropin releasing hormone receptors derived from quinolone-6-carboxamides. Bioorganic and Medicinal Chemistry Letters, 10(5), 443-447. https://doi.org/10.1016/S0960-894X(00)00024-X

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title = "Potent antagonists of gonadotropin releasing hormone receptors derived from quinolone-6-carboxamides",

abstract = "SAR studies which focused upon the C-6 position of a recently described series of quinolone gonadotropin releasing hormone antagonists are reported. Synthetic access to diverse quinolone-6-carboxamides was achieved via the palladium-catalyzed amino-carbonylation reactions of iodide 4 with various amines. Amides related to 9y were especially potent, functional antagonists of rat and human GnRH receptors. (C) 2000 Elsevier Science Ltd. All rights reserved.",

author = "Walsh, {Thomas F.} and Toupence, {Richard B.} and Young, {Jonathan R.} and Huang, {Song X.} and Feroze Ujjainwalla and Devita, {Robert J.} and Goulet, {Mark T.} and Wyvratt, {Matthew J.} and Fisher, {Michael H.} and Lo, {Jane Ling} and Ning Ren and Yudkovitz, {Joel B.} and Yang, {Yi Tien} and Kang Cheng and Smith, {Roy G.}",

year = "2000",

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language = "English",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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Walsh, TF, Toupence, RB, Young, JR, Huang, SX, Ujjainwalla, F, Devita, RJ, Goulet, MT, Wyvratt, MJ, Fisher, MH, Lo, JL, Ren, N, Yudkovitz, JB, Yang, YT, Cheng, K & Smith, RG 2000, 'Potent antagonists of gonadotropin releasing hormone receptors derived from quinolone-6-carboxamides', Bioorganic and Medicinal Chemistry Letters, vol. 10, no. 5, pp. 443-447. https://doi.org/10.1016/S0960-894X(00)00024-X

TY - JOUR

T1 - Potent antagonists of gonadotropin releasing hormone receptors derived from quinolone-6-carboxamides

AU - Walsh, Thomas F.

AU - Toupence, Richard B.

AU - Young, Jonathan R.

AU - Huang, Song X.

AU - Ujjainwalla, Feroze

AU - Devita, Robert J.

AU - Goulet, Mark T.

AU - Wyvratt, Matthew J.

AU - Fisher, Michael H.

AU - Lo, Jane Ling

AU - Ren, Ning

AU - Yudkovitz, Joel B.

AU - Yang, Yi Tien

AU - Cheng, Kang

AU - Smith, Roy G.

PY - 2000/3/6

Y1 - 2000/3/6

N2 - SAR studies which focused upon the C-6 position of a recently described series of quinolone gonadotropin releasing hormone antagonists are reported. Synthetic access to diverse quinolone-6-carboxamides was achieved via the palladium-catalyzed amino-carbonylation reactions of iodide 4 with various amines. Amides related to 9y were especially potent, functional antagonists of rat and human GnRH receptors. (C) 2000 Elsevier Science Ltd. All rights reserved.

AB - SAR studies which focused upon the C-6 position of a recently described series of quinolone gonadotropin releasing hormone antagonists are reported. Synthetic access to diverse quinolone-6-carboxamides was achieved via the palladium-catalyzed amino-carbonylation reactions of iodide 4 with various amines. Amides related to 9y were especially potent, functional antagonists of rat and human GnRH receptors. (C) 2000 Elsevier Science Ltd. All rights reserved.

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U2 - 10.1016/S0960-894X(00)00024-X

DO - 10.1016/S0960-894X(00)00024-X

M3 - Article

C2 - 10743944

AN - SCOPUS:0034611086

SN - 0960-894X

VL - 10

SP - 443

EP - 447

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 5

ER -

Potent antagonists of gonadotropin releasing hormone receptors derived from quinolone-6-carboxamides

Abstract

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