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    Seryl-lysyl-based peptide and peptidomimetic inhibitors of N-myristoyl transferase as anti-infective agents
    7.
    发明授权
    Seryl-lysyl-based peptide and peptidomimetic inhibitors of N-myristoyl transferase as anti-infective agents 失效
    作为抗感染剂的N-肉豆蔻酰基转移酶的丝氨酰赖氨酰基肽和肽模拟抑制剂

    公开(公告)号：US5942600A

    公开(公告)日：1999-08-24

    申请号：US823101

    申请日：1997-03-24

    申请人： James A. Sikorski ,  Balekudru Devadas ,  Daniel P. Getman ,  David L. Brown ,  Srinivasan Nagarajan ,  Mark E. Zupec ,  Jeffrey I. Gordon

    发明人： James A. Sikorski ,  Balekudru Devadas ,  Daniel P. Getman ,  David L. Brown ,  Srinivasan Nagarajan ,  Mark E. Zupec ,  Jeffrey I. Gordon

    IPC分类号： A61K38/00 ,  C07K5/06 ,  C07K5/083 ,  A61K38/06

    CPC分类号： C07K5/06191 ,  C07K5/0606 ,  C07K5/081 ,  A61K38/00

    摘要： Seryl-lysyl-based peptide and peptidomimetic compounds are described as inhibitors of the enzyme N-myristoyl transferase to provide selective control of the fungal organism Candida albicans. Peptidomimetic compounds of particular interest are those of the formula: ##STR1## wherein R.sup.1 is selected form aminoalkyl, p-aminoalkylphenylalkyl, imidazolylalkylphenylalkyl, 2-alkylimidazolylalkylphenylalkyl, benzimidazolylalkylphenylalkyl and 2-alkylbenzimidazolylalkylphenylalkyl; wherein R.sup.2 is selected from hydrido, alkyl, cycloalkyl, akenyl, alkynyl, haloalkyl, benzyl, alkylphenylalkyl, alkoxyphenylalkyl, halophenylalkyl, phenethyl, cycloalkylalkyl, halocycloalkylalkyl, alkylcycloalkylalkyl, alkoxycycloalkylalkyl and naphthylalkyl; wherein Y is selected from carboxylic acid, hydroxamic acid, phosphonic acid and tetrazolyl; or a pharmaceutically-acceptable salt, amide or ester thereof. Compounds of the formula are species-specific inhibitors of C. albicans with little effect on human NMT enzyme and thus would be useful in treating C. albicans fungal infections in humans.

    摘要翻译： 基于丝氨酰赖氨酰的肽和拟肽化合物被描述为N-肉豆蔻酰转移酶的抑制剂，以提供真菌生物体白色念珠菌的选择性控制。 特别感兴趣的拟肽化合物是下式的化合物：其中R1选自氨基烷基，对氨基烷基苯基烷基，咪唑基烷基苯基烷基，2-烷基咪唑基烷基苯基烷基，苯并咪唑基烷基苯基烷基和2-烷基苯并咪唑基烷基苯基烷基; 烷基，环烷基，烯基，炔基，卤代烷基，苄基，烷基苯基烷基，烷氧基苯基烷基，卤代苯基烷基，苯乙基，环烷基烷基，卤代环烷基烷基，烷基环烷基烷基，烷氧基环烷基烷基和萘基烷基。 其中Y选自羧酸，异羟肟酸，膦酸和四唑基; 或其药学上可接受的盐，酰胺或酯。 式的化合物是白色念珠菌的物种特异性抑制剂，对人NMT酶几乎没有影响，因此可用于治疗人类白色念珠菌真菌感染。