Synthesis and pharmacological evaluation of potential metabolites of the potassium-competitive acid blocker BYK 405879 |
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| Authors: | Andreas Marc Palmer Gabriela Münch Wolfgang Kromer |
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| Institution: | a NYCOMED GmbH, Department of Medicinal Chemistry, Byk-Gulden-Str. 2, D-78467 Konstanz, Germany
b NYCOMED GmbH, Department of Pharmacology, Byk-Gulden-Str. 2, D-78467 Konstanz, Germany |
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| Abstract: | Four potential metabolites of the potassium-competitive acid blocker BYK 405879 (1) were synthesized which might be formed in vivo by enzymatic oxidation of the pyran moiety or the methyl groups attached to the (hetero) aromatic system. In all cases, the oxidation of the parent compound 1 was accompanied by a significant loss of pharmacological activity and by a decrease in lipophilicity. The target compounds 6, 14, 20, and 21 constitute valuable tool substances for the investigation of the metabolic fate of BYK 405879 (1). |
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| Keywords: | Phase I metabolism Potassium-competitive acid blocker Pharmacological activity Synthesis of potential metabolites |
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