Title of article
Synthesis and pharmacological evaluation of potential metabolites of the potassium-competitive acid blocker BYK 405879
Author/Authors
Palmer، نويسنده , , Andreas Marc and Münch، نويسنده , , Gabriela and Grobbel، نويسنده , , Burkhard and Kromer، نويسنده , , Wolfgang، نويسنده ,
Issue Information
هفته نامه با شماره پیاپی سال 2009
Pages
3
From page
3917
To page
3919
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).
Keywords
Phase I metabolism , Potassium-competitive acid blocker , Pharmacological activity , Synthesis of potential metabolites
Journal title
Tetrahedron Letters
Serial Year
2009
Journal title
Tetrahedron Letters
Record number
1864775
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