ISSN:
0018-019X
Keywords:
Chemistry
;
Organic Chemistry
Source:
Wiley InterScience Backfile Collection 1832-2000
Topics:
Chemistry and Pharmacology
Notes:
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 A2, Table 1) fulfil the requirements for a clinical candidate, being orally active, specific, reversible, and relatively short-acting. The chemical work involved is illustrated by describing a choice of exemplary syntheses, dealing with compounds 9, 11, 14, 18, 22, 24, 25, 35, 41, and 42 (Chapt. 5, Schemes 1-10).
Additional Material:
7 Tab.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1002/hlca.19890720511
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