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  • Title: 5-Lipoxygenase inhibitors: convenient synthesis of 4-[3-(4-heterocyclylphenylthio)phenyl]-3,4,5,6-tetrahydro-2H-pyran-4-carboxamide analogues.
    Author: Mano T, Stevens RW, Okumura Y, Kawai M, Okumura T, Sakakibara M.
    Journal: Bioorg Med Chem Lett; 2005 May 16; 15(10):2611-5. PubMed ID: 15863327.
    Abstract:
    A convenient synthetic route to 4-[3-(4-heterocyclylphenylthio)phenyl]-3,4,5,6-tetrahydro-2H-pyran-4-carboxamide analogues as 5-LO inhibitors is described. This methodology enabled rapid development of structure-activity relationships (SARs) leading to improvement of pharmacological properties. Thus, new compounds with higher 5-LO inhibitory potency were discovered. The stereo-chemistry requirements of the tetrahydropyran ring are also discussed.
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