申请人:G. D. Searle & Co.
公开号:US05599947A1
公开(公告)日:1997-02-04
Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitriles thereof. These compounds are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, and as anti-viral and anti-fungal agents or pro-drugs of such agents. Illustrative of the disclosed compounds are fatty acid amino acid analogs of the structure ##STR1## in which X is the ethyl or t-butyl ester of an amino acid such as Gly, L--Ala, L--Ile, L--Phe, L--Trp, L--Thr or an amide such as NHCH.sub.2 C.sub.6 H.sub.5 or NH(CH.sub.2).sub.2 C.sub.6 H.sub.5,
脂肪酸类似物的新衍生物,其脂肪酸部分含有一到三个杂原子,可以是氧、硫或氮,其中羧基末端已经被改性以形成各种酰胺、酯、酮、醇、醇酯和腈。这些化合物可用作N-肉豆蔻酰转移酶(NMT)及/或其酰辅酶的底物,以及抗病毒和抗真菌剂或这些剂的前药。所披露的化合物的示例是脂肪酸氨基酸类似物,其结构为##STR1##其中X是氨基酸(如甘氨酸、L-丙氨酸、L-异亮氨酸、L-苯丙氨酸、L-色氨酸、L-苏氨酸)的乙酯或叔丁基酯,或者是NHCH.sub.2 C.sub.6 H.sub.5或NH(CH.sub.2).sub.2 C.sub.6 H.sub.5等酰胺。