New peptidomimetics in the chemistry of fibrinogen receptor antagonists

被引:10
作者
Gante, J [1 ]
Juraszyk, H [1 ]
Raddatz, P [1 ]
Wurziger, H [1 ]
BernotatDanielowski, S [1 ]
Melzer, G [1 ]
Rippmann, F [1 ]
机构
[1] MERCK KGAA,DEPT PRECLIN PHARMACEUT RES,D-64271 DARMSTADT,GERMANY
来源
LETTERS IN PEPTIDE SCIENCE | 1995年 / 2卷 / 3-4期
关键词
RGD; antithrombotics; GP IIb/IIIa;
D O I
10.1007/BF00119139
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 [生物化学与分子生物学]; 081704 [应用化学];
摘要
RGD-peptidomimetics are currently being investigated as a class of potential antithrombotics that antagonize the fibrinogen receptor, GP IIb/IIIa, on the surface of platelets. These mimetics are expected to have decisive advantages - such as higher activity and specificity, oral bioavailability and longer duration of action - over known antithrombotics. For further optimization in this respect, novel peptidomimetic CP IIb/IIIa antagonists with an oxazolidinonemethyl central building block were synthesized. This building block proved to be very versatile as an 'anchor' for structurally different C-termini and was the starting point for highly efficient and orally active compounds.
引用
收藏
页码:135 / 140
页数:6
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