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A new class of bradykinin antagonists: synthesis and in vitro activity of bissuccinimidoalkane peptide dimers

JC Cheronis, ET Whalley, KT Nguyen…

文献索引:Cheronis, John C.; Whalley, Eric T.; Nguyen, Khe T.; Eubanks, Shad R.; Allen, Lisa G.; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 9 p. 1563 - 1572

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被引用次数: 114

摘要

> 2> 1> 0>> 4, 7, 8, 9. Evaluation of the linker length as represented by the number of methylene units indicated an optimal distance between the two monomeric peptides of six to eight methylene moieties. These studies also revealed that the carbon-chain length significantly affected the duration of action in vitro and resulted in partial agonism effects when n> 8. The optimum activity in vitro was achieved with dimerization at position 6 and ...