Solid-phase synthesis and structure-activity relationships of novel biarylethers as melanin-concentrating hormone receptor-1 antagonists

Vu Ma; Anthony W. Bannon; Jamie Baumgartner; Clarence Hale; Faye Hsieh; Christopher Hulme; Kirk Rorrer; John Salon; Carlo van Staden; Paul Tempest

doi:10.1016/j.bmcl.2006.07.040

Solid-phase synthesis and structure-activity relationships of novel biarylethers as melanin-concentrating hormone receptor-1 antagonists

Vu Ma, Anthony W. Bannon, Jamie Baumgartner, Clarence Hale, Faye Hsieh, Christopher Hulme, Kirk Rorrer, John Salon, Carlo van Staden, Paul Tempest

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

7 Scopus citations

Abstract

Melanin-concentrating hormone (MCH) is a cyclic 19 amino acid orexigenic neuropeptide. The action of MCH on feeding is thought to involve the activation of its respective G protein-coupled receptor MCH-R1. Consequently, antagonists that block MCH regulated MCH-R1 activity may provide a viable approach to the treatment of diet-induced obesity. This communication reports the discovery of a novel MCH-R1 receptor antagonist, the biarylether 7, identified through high throughput screening. The solid-phase synthesis and structure-activity relationship of related analogs is described.

Original language	English (US)
Pages (from-to)	5066-5072
Number of pages	7
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	16
Issue number	19
DOIs	https://doi.org/10.1016/j.bmcl.2006.07.040
State	Published - Oct 1 2006
Externally published	Yes

Keywords

Biarylethers
MCH-R1 antagonists

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmcl.2006.07.040

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Ma, V., Bannon, A. W., Baumgartner, J., Hale, C., Hsieh, F., Hulme, C., Rorrer, K., Salon, J., Staden, C. V., & Tempest, P. (2006). Solid-phase synthesis and structure-activity relationships of novel biarylethers as melanin-concentrating hormone receptor-1 antagonists. Bioorganic and Medicinal Chemistry Letters, 16(19), 5066-5072. https://doi.org/10.1016/j.bmcl.2006.07.040

Ma, V, Bannon, AW, Baumgartner, J, Hale, C, Hsieh, F, Hulme, C, Rorrer, K, Salon, J, Staden, CV & Tempest, P 2006, 'Solid-phase synthesis and structure-activity relationships of novel biarylethers as melanin-concentrating hormone receptor-1 antagonists', Bioorganic and Medicinal Chemistry Letters, vol. 16, no. 19, pp. 5066-5072. https://doi.org/10.1016/j.bmcl.2006.07.040

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abstract = "Melanin-concentrating hormone (MCH) is a cyclic 19 amino acid orexigenic neuropeptide. The action of MCH on feeding is thought to involve the activation of its respective G protein-coupled receptor MCH-R1. Consequently, antagonists that block MCH regulated MCH-R1 activity may provide a viable approach to the treatment of diet-induced obesity. This communication reports the discovery of a novel MCH-R1 receptor antagonist, the biarylether 7, identified through high throughput screening. The solid-phase synthesis and structure-activity relationship of related analogs is described.",

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AU - Ma, Vu

AU - Bannon, Anthony W.

AU - Baumgartner, Jamie

AU - Hale, Clarence

AU - Hsieh, Faye

AU - Hulme, Christopher

AU - Rorrer, Kirk

AU - Salon, John

AU - Staden, Carlo van

AU - Tempest, Paul

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AB - Melanin-concentrating hormone (MCH) is a cyclic 19 amino acid orexigenic neuropeptide. The action of MCH on feeding is thought to involve the activation of its respective G protein-coupled receptor MCH-R1. Consequently, antagonists that block MCH regulated MCH-R1 activity may provide a viable approach to the treatment of diet-induced obesity. This communication reports the discovery of a novel MCH-R1 receptor antagonist, the biarylether 7, identified through high throughput screening. The solid-phase synthesis and structure-activity relationship of related analogs is described.

KW - Biarylethers

KW - MCH-R1 antagonists

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Solid-phase synthesis and structure-activity relationships of novel biarylethers as melanin-concentrating hormone receptor-1 antagonists

Abstract

Keywords

ASJC Scopus subject areas

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