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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
18
|
| pubmed:dateCreated |
1999-2-2
|
| pubmed:abstractText |
In an effort to increase the thrombin inhibitory activity of a novel series of inhibitors (i.e., 1a), substituents were incorporated at the C-3" position of the C-3 aryl ring (2). Consistent with the X-ray crystallography studies, small hydrophobic groups at the C-3" site (Br and Me) enhanced thrombin inhibitory activity by 8-fold. However, a few more hydrophilic substituents (NO2 and OMe) also enhanced the potency of the series. The biological results are discussed in terms of molecular modeling studies.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Sep
|
| pubmed:issn |
0960-894X
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:day |
22
|
| pubmed:volume |
8
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
2527-32
|
| pubmed:dateRevised |
2000-12-18
|
| pubmed:meshHeading |
pubmed-meshheading:9873574-Binding Sites,
pubmed-meshheading:9873574-Crystallography, X-Ray,
pubmed-meshheading:9873574-Models, Chemical,
pubmed-meshheading:9873574-Models, Molecular,
pubmed-meshheading:9873574-Serine Proteinase Inhibitors,
pubmed-meshheading:9873574-Structure-Activity Relationship,
pubmed-meshheading:9873574-Thiophenes,
pubmed-meshheading:9873574-Thrombin
|
| pubmed:year |
1998
|
| pubmed:articleTitle |
Dibasic benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors. 2. Exploring interactions at the proximal (S2) binding site.
|
| pubmed:affiliation |
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA.
|
| pubmed:publicationType |
Journal Article
|