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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
26
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pubmed:dateCreated |
1997-1-24
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pubmed:abstractText |
As reported in our previous paper, a series of indole-3-acetamides which possessed potency and selectivity as inhibitors of human nonpancreatic secretory phospholipase A2(hnps-PLA2) was developed. The design of these compounds was based on information derived from x-ray crystal structures determined for complexes between the enzyme and its inhibitors. We describe here the further implementation of this structure-based design strategy and continued SAR development to produce indole-3-acetamides with additional functionalities which provide increased interaction with important residues within the enzyme active site. These efforts led to inhibitors with substantially enhanced potency and selectivity.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:AsayJ LJL,
pubmed-author:CENEKRR,
pubmed-author:CarlsonD GDG,
pubmed-author:ChirgadzeN YNY,
pubmed-author:ClawsonD KDK,
pubmed-author:DillardR DRD,
pubmed-author:DraheimS ESE,
pubmed-author:HartleyL WLW,
pubmed-author:JohnsonL MLM,
pubmed-author:JonesN DND,
pubmed-author:McKinneyE RER,
pubmed-author:MihelichE DED,
pubmed-author:OlkowskiJ LJL,
pubmed-author:SchevitzR WRW,
pubmed-author:SmithA CAC,
pubmed-author:SnyderD WDW,
pubmed-author:SommersC DCD,
pubmed-author:WeryJ PJP
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pubmed:issnType |
Print
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pubmed:day |
20
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|
pubmed:volume |
39
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5137-58
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
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pubmed:year |
1996
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pubmed:articleTitle |
Indole inhibitors of human nonpancreatic secretory phospholipase A2. 2. Indole-3-acetamides with additional functionality.
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pubmed:affiliation |
Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana 46285, USA.
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pubmed:publicationType |
Journal Article
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