4-[4-[(2-Hydroxybenzoyl) amino] phenyl] butyric acid as a novel oral delivery agent for recombinant human growth hormone

…, C Lercara, S Milstein, D O'Toole…

文献索引：Leone-Bay, Andrea; Ho, Koc-Kan; Agarwal, Rajesh; Baughman, Robert A.; Chaudhary, Kiran; DeMorin, Frenel; Genoble, Lise; McInnes, Campbell; Lercara, Christine; Milstein, Sam; O'Toole, Doris; Sarubbi, Donald; Variano, Bruce; Paton, Duncan R. Journal of Medicinal Chemistry, 1996 , vol. 39, # 13 p. 2571 - 2578

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被引用次数: 122

摘要

A series of N-acetylated, non-α, aromatic amino acids was prepared and shown to promote the absorption of recombinant human growth hormone (rhGH) from the gastrointestinal tract. Seventy compounds in this family were tested in vivo in rats. Of the compounds tested, 4-[4- [(2-hydroxybenzoyl) amino] phenyl] butyric acid was identified as a preclinical candidate and was used to demonstrate the oral delivery of rhGH in primates. A significant positive ...