Potent and selective 5-LO inhibitor bearing benzothiophene pharmacophore: discovery of MK-5286 |
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| Authors: | Li Lianhai Berthelette Carl Chateauneuf Anne Ouellet Marc Sturino Claudio F Wang Zhaoyin |
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| Institution: | Department of Medicinal Chemistry, Merck Frosst Centre for Therapeutic Research, Kirkland, Québec, Canada. lianhai_li@merck.com |
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| Abstract: | The strategy and SAR studies that led to the discovery of a novel potent and orally available 5-lipoxygenase (5-LO) inhibitor 3-(4-fluorophenyl)-6-({4-(1S)-1-hydroxy-1-(trifluoromethyl)propyl]-1H-1,2,3-triazol-1-yl}methyl)-1-benzothiophene-2-carboxamide ((S)-2l or MK-5286) were described. |
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