Catechol??O??methyltransferase??inhibiting pyrocatechol derivatives: synthesis and structure??activity studies

J Borgulya, H Bruderer, K Bernauer…

文献索引：Borgulya; Bruderer; Bernauer; Zurcher; Da Prada Helvetica Chimica Acta, 1989 , vol. 72, # 5 p. 952 - 968

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被引用次数: 117

摘要

Abstract 3-Nitro-and 3-cyanopyrocatechols bearing electron-withdrawing substituents at C (5) have been found to inhibit the enzyme catechol-O-methyltransferase. Structure-activity studies are discussed on the basis of the pharmocological data of 50 compounds (cf, Chapt. 4, Tables 1–7). Some 3-nitro-5-aroylpyrocatechols (Type A 2, Table 1) fulfil the requirements for a clinical candidate, being orally active, specific, reversible, and relatively short-acting. ...