Literature DB >> 10636236

6-Acylamino-2-[(alkylsulfonyl)oxy]-1H-isoindole-1,3-dione mechanism-based inhibitors of human leukocyte elastase.

J E Kerrigan1, M C Walters, K J Forrester, J B Crowder, L J Christopher.   

Abstract

A study of various 2-[(alkylsulfonyl)oxy]-6-substituted-1H-isoindole-1,3-diones' inhibition of chymotrypsin compared to inhibition of HLE reveals that acylamino substitution in the 6-position increases selectivity and potency of these inhibitors for HLE. The best HLE inhibitor in this series was 6-(methylglutaryl)amino-2-[(ethylsulfonyl)oxy]-1H-isoindole-1,3-di one with a kobs/[I] = 220,000 M(-1) s(-1).

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Year:  2000        PMID: 10636236     DOI: 10.1016/s0960-894x(99)00588-0

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  2-(2-Iodo-phen-yl)isoindoline-1,3-dione.

Authors:  Güneş Demirtaş; Necmi Dege; Ayşen Alaman Ağar; Orhan Büyükgüngör
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-03-12
  1 in total

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