Title of article
Potency and selectivity of P2/P3-modified inhibitors of cysteine proteases from trypanosomes
Author/Authors
Priyadarshini Jaishankar، نويسنده , , Elizabeth Hansell، نويسنده , , Dongmei Zhao، نويسنده , , Patricia S. Doyle، نويسنده , , Andrej Sali and James H. McKerrow، نويسنده , , Adam R. Renslo، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
624
To page
628
Abstract
A systematic study of P2 and P3 substitution in a series of vinyl sulfone cysteine protease inhibitors is described. The introduction of a methyl substituent in the P2 phenylalanine aryl ring had a favorable effect on protease inhibition and conferred modest selectivity for rhodesain over cruzain. Rhodesain selectivity could be enhanced further by combining these P2 modifications with certain P3 amide substituents.
Keywords
Cysteine protease inhibitors , Trypanosomes , Vinyl sulfones , cysteine proteases , Antiparasitics , Antitrypanosomals
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799027
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