84903-82-2Relevant articles and documents
Synthesis of potential drug metabolites by a modified Udenfriend reaction
Slavik, Roger,Peters, Jens-Uwe,Giger, Rudolf,Bürkler, Markus,Bald, Eric
experimental part, p. 749 - 752 (2011/03/21)
The scope and the limitations of a modified Udenfriend reaction for the one-step synthesis of potential drug metabolites were explored. Several drugs (clozapine, chlorpromazine, imipramine, buspirone, diltiazem, and propranolol) were subjected to modified Udenfriend conditions (Fe2+/Mn 2+/EDTA/ascorbic acid/O2). From each reaction, one to four oxidation products were obtained in 1-8% overall yield. Many of these products (9 out of 14) have been reported to be metabolites of the parent drugs in vivo. The products resulted mainly from aromatic hydroxylation, and are not readily accessible by conventional synthesis. Thus, the described reaction may be useful in drug discovery whenever a facile synthetic access is more important than high yields (e.g., for a fast derivatisation of compounds or the preparation of metabolites). Poorly water-soluble compounds cannot be converted, which is an important limitation of this method. 2010 American Chemical Society.
Methods For Treating A Condition Characterized By Dysfunction In Protein Homeostasis
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, (2009/08/18)
Methods are provided for treating conditions characterized by dysfunction in protein homeostasis in a patient in need thereof. A method for treating a condition characterized by dysfunction in protein homeostasis in a patient in need thereof is provided which comprises administering to the patient a proteostasis regulator in an amount effective to improve or restore protein homeostasis, and to reduce or eliminate the condition in the patient or to prevent its occurrence or recurrence. The condition can be a loss of function disorder such as a lysosomal storage disease, or a gain of function disorder such as an aging associated disease.
