Combinatorial library of substituted statine esters and amides via a novel acid-catalyzed rearrangement
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United States of America Patent
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Jul 3, 2001
Grant Date -
N/A
app pub date -
May 15, 1998
filing date -
Apr 14, 1997
priority date (Note) -
Expired
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Abstract
A combinatorial chemical library comprising a plurality of members of the Formula [S]--C(O)--L'-Z containing hydroxyamides is disclosed, in which [S] represents a solid support and L'-Z is a linker/compound residue. In this library, Z is ##STR1## and Y is --NR.sup.3 R.sup.4 or --OR.sup.9. R.sup.3 and R.sup.4 are independently selected from the group consisting of H, alkyl, aralkyl, heteroarylalkyl, heterocycloalkyl, --CH(R.sup.5)CH(R.sup.6)OH, --CH(R.sup.5)C(O)NHR.sup.6 and --CH(R.sup.5)C(O)NHCH(R.sup.6)C(O)NHR.sup.7. R.sup.3 and R.sup.4 together are ##STR2## wherein X=O or NR.sup.8 and R.sup.9 is aryl, aralkyl or R.sup.7 CH.dbd.CH(CH.sub.2).sub.n. The combinatorial library can be optionally encoded with identifiers T'-L, which are covalently attached to the solid support. The methods of synthesizing such a library are described. The use of such library in assays to discover biologically active compounds is also disclosed.
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