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Discovery of cyclopentane- and cyclohexane-trans-1,3-diamines as potent melanin-concentrating hormone receptor 1 antagonists
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2007 (English)In: Bioorganic & Medicinal Chemistry Letters, Vol. 17, no 15, 4232-41 p.Article in journal (Refereed) Published
Abstract [en]

We herein report the optimization of cyclopentane- and cyclohexane-1,3-diamine derivatives as novel and potent MCH-R1 antagonists. Structural modifications of the 2-amino-quinoline and thiophene moieties found in the initial lead compound served to improve its metabolic stability profile and MCH-R1 affinity, and revealed unprecedented SAR when compared to other 2-amino-quinoline-containing MCH-R1 antagonists.

Place, publisher, year, edition, pages
2007. Vol. 17, no 15, 4232-41 p.
Keyword [en]
Melanin-concentrating hormone receptor; MCH, MCH-R1 antagonists, Obesity
Identifiers
URN: urn:nbn:se:umu:diva-16155DOI: doi:10.1016/j.bmcl.2007.05.034OAI: oai:DiVA.org:umu-16155DiVA: diva2:155828
Available from: 2007-08-21 Created: 2007-08-21 Last updated: 2011-01-11Bibliographically approved

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