Document Report Card

ID: ALA1121736

Journal: J Med Chem

Title: Synthesis and evaluation of some stable multisubstrate adducts as inhibitors of catechol O-methyltransferase.

Authors: Anderson GL, Bussolotti DL, Coward JK.

Abstract: A new series of methylase inhibitors has been designed in which the nucleophilic methyl acceptor is attached to the adenosine and/or homocysteine fragments of the methyl donor, S-adenosylmethionine, to form a "multisubstrate adduct". In the present case, catecholamine analogues attached through a phenethyl sulfide linkage to 5'-thioadenosine or homocysteine have been synthesized, together with the corresponding methylsulfonium salts. These compounds were assayed as inhibitors of catechol O-methyltransferase, and the adenosylsulfonium salts (4) were found to be inhibitors of the enzyme.

CiteXplore: 7310802

DOI: 10.1021/jm00143a002