Dipartimento di Chimica Organica e Industriale, Universita' degli Studi di Milano, Via Venezian, 21, Milano, Italy.
Curr Med Chem. 2010;17(3):264-89. doi: 10.2174/092986710790149729.
In recent years, phosphonic acids and their derivatives have received increasing attention as analogues of a series of naturally occurring phosphates and as "bio-isosteric phosphorus analogues" of amino acids. Unlike a phosphate group, the phosphonate moiety is not readily hydrolyzed, in a biological environment, by the enzymes involved in the phosphate cleavage. This feature makes these compounds extremely useful in several applications, in metabolic regulation, in enhancement or inhibition studies, in the development of potential drugs against several metabolic disorders. The great potential of these compounds in biological applications resulted in an intense effort directed to the development of efficient synthetic methods for their preparation, with particular attention to stereoselective synthesis. The purpose of this review is to give an up-to-date account of the chemistry, the synthesis and the biological activity of aminophosphonic acids and their derivatives.
近年来，膦酸及其衍生物作为一系列天然存在的磷酸盐的类似物以及氨基酸的“生物等排磷类似物”受到越来越多的关注。与磷酸基团不同，膦酸酯部分在涉及磷酸裂解的酶存在下不易在生物环境中水解。这一特性使这些化合物在几种应用中非常有用，例如代谢调节、增强或抑制研究、开发针对几种代谢紊乱的潜在药物。这些化合物在生物应用中的巨大潜力促使人们致力于开发其制备的有效合成方法，特别关注立体选择性合成。本文综述了氨基膦酸及其衍生物的化学、合成和生物活性。
