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Journal of Enzyme Inhibition and Medicinal Chemistry Volume 25, 2010 - Issue 1
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Short Communication

Synthesis and activity of amides of tripeptides as potential urokinase inhibitors

Agnieszka MarkowskaDepartment of Organic Chemistry, Medical University of Bialystok, Bialystok, PolandCorrespondence[email protected]
,
Irena BruzgoDepartment of Organic Chemistry, Medical University of Bialystok, Bialystok, Poland
&
Krystyna Midura-NowaczekDepartment of Organic Chemistry, Medical University of Bialystok, Bialystok, Poland
Pages 139-142 | Received 03 Feb 2009, Accepted 23 Apr 2009, Published online: 23 Dec 2009
 
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Abstract

Eleven peptides of the general formula H-d-Ser-Ala-Arg-NH-X, where X = (CH2)n-NH2, n = 2–9, (CH2)m-OH, m = 2–4, were obtained and tested for their effect on the amidolytic activities of urokinase, thrombin, trypsin, plasmin, t-PA, and kallikrein. H-d-Ser-Ala-Arg-NH-(CH2)5-NH2 inhibited urokinase with a Ki value of 6.3 μM.

Acknowledgements

Declaration of interest: The authors report no conflicts of interest.

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