New peptidomimetics in the chemistry of fibrinogen receptor antagonists
New peptidomimetics in the chemistry of fibrinogen receptor antagonists
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DOI：
10.1007/bf00119139
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发表时间：
1995-11-01
期刊：
影响因子：
--
通讯作者：
Rippmann, F
中科院分区：
文献类型：
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作者：
Gante, J;Juraszyk, H;Rippmann, F
目前正在研究的RGD-肽模拟物作为一类潜在的抗血栓药，拮抗血小板表面的纤维蛋白原受体，GP IIb/IIIa。这些模拟物预计具有决定性的优势-如更高的活性和特异性，口服生物利用度和更长的作用持续时间-超过已知的抗血栓药物。为了在这方面进一步优化，合成了具有恶唑烷酮甲基中心结构单元的新型拟肽CP IIb/IIIa拮抗剂。这种结构单元被证明是非常通用的，作为结构上不同的C-末端的“锚”，并且是高效和口服活性化合物的起点。
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.