Novel 3-phenylprop-2-ynylamines as inhibitors of mammalian squalene epoxidase |
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| Authors: | Musso David L Clarke Morris J Kelley James L Boswell G Evan Chen Grace |
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| Affiliation: | GlaxoSmithKline Research and Development, Five Moore Dr., Research Triangle Park, NC 27709, USA. Dave.L.Musso@gsk.com |
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| 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 microM against rat liver squalene epoxidase. Against 23 strains of fungal squalene epoxidase compound 19 was found to be inactive. |
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