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Inhibition of human leukocyte elastase. 1. Inhibition by C-7-substituted cephalosporin tert-butyl esters
Journal of Medicinal Chemistry1990Vol. 33(9), pp. 2513–2521
Citations Over TimeTop 10% of 1990 papers
James B. Doherty, Bonnie M. Ashe, Peter L. Barker, Thomas J. Blacklock, John W. Butcher, Gilbert O. Chandler, Mary Ellen Dahlgren, Philip R. Davies, Conrad P. Dorn
Abstract
Time-dependent inhibitors of the enzyme human leukocyte elastase have been developed based on the cephem nucleus. A series of cephalosporin tert-butyl esters has been examined, and the activity of these compounds has been found to be very sensitive to C-7 substituents, with small, alpha-oriented, electron-withdrawing groups showing greatest activity. Additionally, the oxidation state of the sulfur atom has been found to play a role in potency, with sulfones showing considerably greater activity than the corresponding sulfides or beta-sulfoxides. The alpha-sulfoxides were inactive.
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