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

The designed and synthesized anticoagulant activity and structure-activity relationship of a series of low molecular weight peptide inhibitors of Factor Xa, fragment analogues of ATS and GLS, is reported. The newly synthesized peptides have the following structure: H-X-Pro-Lys-Arg-Lys-Leu-Val-Pro-Y (X = Arg, Lys, Orn or missed and Y = OH, NH2).