Linked Life Data

10445044

Source:http://linkedlifedata.com/resource/pubmed/id/10445044

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
3
pubmed:dateCreated
1999-9-9
pubmed:abstractText
A series of new analogs with modifications in the C-terminal residue were prepared based on the known thrombin inhibitor D-Phe-Pro-agmatine. These include several compounds alkylated at the N delta-, N omega- and N omega'-atoms of the guanidino group and a number of inhibitors derived from commercially available diamines. All analogs with alkylation of the guanidino group showed very poor activity. In contrast, the most potent and selective inhibitor with a cyclic and basic residue in the P1-position was found to be Ph-CH2-SO2-D-Cha-Pro-4-(amidomethyl) amidinopiperidine 11 with a Ki of 0.27 nM. In addition, a number of compounds were synthesized, in which the basic amidino group of the P1-residue was replaced by a hydroxyl group. Although the inhibition constants of these phenol derivatives showed still remarkable potency (16, Ki = 130 nM), their activity in clotting assays was strongly reduced.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
8755-5093
pubmed:author
pubmed:issnType
Print
pubmed:volume
14
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
203-16
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1999
pubmed:articleTitle
New thrombin inhibitors based on D-cha-Pro-derivatives.
pubmed:affiliation
Inst. of Biochemistry & Biophysics, Friedrich Schiller University, Jena, Germany. steinmetzer@merlin.biologie.uni-jena.de
pubmed:publicationType
Journal Article, Comparative Study