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rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
18
|
|
pubmed:dateCreated |
1999-2-2
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|
pubmed:abstractText |
Potent serine protease inhibitor 1a featuring a hybrid P3-P4 quaternary lactam dipeptide surrogate was prepared based upon SAR and molecular modeling investigations and in order to further probe the S2/S3 thrombin and FXa subsites. An efficient and concise synthetic route to the key aminolactam intermediate 4 was developed. The design, synthesis, and biological activity of this target and its P3-P4 diastereomer 1b is presented.
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pubmed:language |
eng
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pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Sep
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|
pubmed:issn |
0960-894X
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|
pubmed:author |
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
22
|
|
pubmed:volume |
8
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
2501-6
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|
pubmed:dateRevised |
2006-11-15
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|
pubmed:meshHeading |
pubmed-meshheading:9873569-Chromatography, High Pressure Liquid,
pubmed-meshheading:9873569-Dipeptides,
pubmed-meshheading:9873569-Guanidines,
pubmed-meshheading:9873569-Humans,
pubmed-meshheading:9873569-Lactams,
pubmed-meshheading:9873569-Magnetic Resonance Spectroscopy,
pubmed-meshheading:9873569-Models, Chemical,
pubmed-meshheading:9873569-Models, Molecular,
pubmed-meshheading:9873569-Molecular Structure,
pubmed-meshheading:9873569-Piperidines,
pubmed-meshheading:9873569-Serine Proteinase Inhibitors,
pubmed-meshheading:9873569-Structure-Activity Relationship,
pubmed-meshheading:9873569-Thrombin
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|
pubmed:year |
1998
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|
pubmed:articleTitle |
Design and construction of novel thrombin inhibitors featuring P3-P4 quaternary lactam dipeptide surrogates.
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|
pubmed:affiliation |
Department of Medicinal Chemistry, Corvas International, Inc., San Diego, CA 92121, USA.
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pubmed:publicationType |
Journal Article,
In Vitro
|
