Design, synthesis and structure-activity relationship of a series of fragment analogues of antistasin (ATS) and ghilantens (GLS).

A series of low molecular weight peptide inhibitors of Factor Xa, fragment analogues of ATS and GLS, was designed and synthesized by the SPPS method. The new analogues included different basic amino acids in 109 position. In order to investigate the role of these factors, the newly synthesized peptides were tested for anticoagulant activity.

Synthesis and structure-activity relationship of new analogues of antistasin.

Intensive investigation connected with the development of new anticoagulant agents for the treatment of cardiovascular diseases was carried out. Direct and specific inhibition of thrombin and Factor Xa-like serine proteases in the coagulation cascade has been the focus of many efforts to design novel anticoagulants over the past decade. This work reports the synthesis and biological activity of new anticoagulant peptide analogues of natural isoforms 2 and 3 of antistasin.