- The fourth molybdenum containing enzyme mARC: Cloning and involvement in the activation of N-hydroxylated prodrugs
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The recently discovered mammalian molybdoprotein mARC1 is capable of reducing N-hydroxylated compounds. Upon reconstitution with cytochrome b 5 and b5 reductase, benzamidoxime, pentamidine, and diminazene amidoximes, N-hydroxymelagatran, guanoxabenz, and N-hydroxydebrisoquine are efficiently reduced. These substances are amidoxime/N-hydroxyguanidine prodrugs, leading to improved bioavailability compared to the active amidines/guanidines. Thus, the recombinant enzyme allows prediction about in vivo reduction of N-hydroxylated prodrugs. Furthermore, the prodrug principle is not dependent on cytochrome P450 enzymes.
- Gruenewald, Sanja,Wahl, Bettina,Bittner, Florian,Hungeling, Helen,Kanzow, Stephanie,Kotthaus, Joscha,Schwering, Ulrike,Mendel, Ralf R.,Clement, Bernd
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scheme or table
p. 8173 - 8177
(2009/12/07)
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- Process for producing amidine sulfonic acids
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An efficient synthesis of quanidines, e.g. of the formula (III), by oxidizing a thiourea, e.g. of the following formula (II): STR1 with H2 O2 and a molybdenum catalyst to yield an aminoiminomethane sulfonic acid which can then be reacted with an amine followed by optional transamination steps.
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