申请人:——
公开号:US20040068094A1
公开(公告)日:2004-04-08
A method for modifying the cyclic peptide ring system of Echinocandin-type compounds to produce new analogs having antifungal activity is provided. The inventive process comprises opening the cyclic peptide ring, cleaving the terminal ornithine unit, inserting at least one new amino acid or other synthetic unit and closing the ring to produce a new cyclic peptide ring structure. The process allows one to incorporate features such as water-solubility into the cyclic peptide ring nucleus, sites for further modification, increase or decrease the number of amino acid or peptide units within the ring nucleus, and increase or decrease the total number of members within the ring. The invention further provides novel Echinocandin type compounds and their use as antifungal or anti-parasitic agents.
本发明提供了一种改变Echinocandin型化合物的环肽环系统以产生具有抗真菌活性的新类似物的方法。该创新过程包括打开环肽环,裂解末端鸟氨酸单元,插入至少一个新的氨基酸或其他合成单元,并闭合环以产生新的环肽环结构。该过程允许将水溶性等特征纳入环肽环核中,为进一步修饰提供位点,增加或减少环核中的氨基酸或肽单元的数量,并增加或减少环中的总成员数。本发明还提供了新型Echinocandin型化合物及其用作抗真菌或抗寄生虫剂的用途。