Phosphonopeptides are mimetics of peptides in which phosphonic acid or related (phosphinic, phosphonous etc.) group replaces either carboxylic acid group present at C-terminus, is located in the peptidyl side chain, or phosphonamidate or phosphinic acid mimics peptide bond. Acting as inhibitors of key enzymes related to variable pathological states they display interesting and useful physiologic activities with potential applications in medicine and agriculture. Since the synthesis and biological properties of peptides containing C-terminal diaryl phosphonates and those with phosphonic fragment replacing peptide bond were comprehensively reviewed, this review concentrate on peptides holding free, unsubstituted phosphonic acid moiety. There are two groups of such mimetics: (i) peptides in which aminophosphonic acid is located at C-terminus of the peptide chain with most of them (including antibiotics isolated from bacteria and fungi) exhibiting antimicrobial activity; (ii) non-hydrolysable analogues of phosphonoamino acids, which are useful tools to study physiologic effects of phosphorylations.

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含有游离膦酸基团的膦肽：最新进展

膦酸肽是膦酸或相关肽（次膦酸、亚膦酸等）的肽的模拟物。) 基团取代存在于 C 末端的羧酸基团，位于肽基侧链，或膦酰胺或次膦酸模拟肽键。作为与可变病理状态相关的关键酶的抑制剂，它们显示出有趣且有用的生理活性，在医学和农业中具有潜在的应用。由于对含有 C 末端膦酸二芳基酯和膦酸片段取代肽键的肽的合成和生物学特性进行了全面综述，因此本综述集中在含有游离、未取代的膦酸部分的肽上。有两组这样的模拟物：(i) 氨基膦酸位于肽链 C 端的肽，其中大部分（包括从细菌和真菌中分离的抗生素）显示出抗菌活性；(ii) 膦酸氨基酸的不可水解类似物，它们是研究磷酸化生理效应的有用工具。