Issue 3, 2003
From the journal:

Organic & Biomolecular Chemistry

Novel 3-phenylprop-2-ynylamines as inhibitors of mammalian squalene epoxidase†

David L. Musso,‡*a   Morris J. Clarke,b   James L. Kelley,c   G. Evan Boswelld  and  Grace Chena  

* Corresponding authors

a GlaxoSmithKline Research and Development, Five Moore Dr., Research Triangle Park, NC 27709
E-mail: Dave.L.Musso@gsk.com

b UNC School of Pharmacy, University of North Carolina at Chapel Hill, Campus Box 7360, Chapel Hill, NC 27599

c 10928 Raven Rock Drive, Raleigh, NC 27614

d Pfizer, 7000 Portage Rd., 1593-91-201, Kalamazoo, MI 49001

Abstract

The synthesis of a novel series of 3-phenylprop-2-ynylamines as selective mammalian squalene epoxidase inhibitors is described. Structure–activity relationship studies led to the discovery of compound 19, 1-[3-(3,5-dichlorophenyl)prop-2-ynyl]-3-methylpiperidine hydrochloride with an IC50 of 2.8 ± 0.6 µM against rat liver squalene epoxidase. Against 23 strains of fungal squalene epoxidase compound 19 was found to be inactive.

Graphical abstract: Novel 3-phenylprop-2-ynylamines as inhibitors of mammalian squalene epoxidase

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Article information

DOI
https://doi.org/10.1039/B209165H
Article type
Paper
Submitted
18 Sep 2002
Accepted
14 Nov 2002
First published
09 Jan 2003

Org. Biomol. Chem., 2003,1, 498-506

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Novel 3-phenylprop-2-ynylamines as inhibitors of mammalian squalene epoxidase

D. L. Musso, M. J. Clarke, J. L. Kelley, G. Evan Boswell and G. Chen, Org. Biomol. Chem., 2003, 1, 498 DOI: 10.1039/B209165H

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