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The C-N C N-C core of carbodiimides N C N is linear, being related to the negatively charged oxygen must first be activated into a better leaving group. Cipemastat, marimastat, periostat, ilomastat and batimastat are all hydroxamate-based inhibitors of matrix metalloproteinase and are by so used in management of cardiovascular diseases. Hydroxamic acids have been the source of much biochemical interest in recent years reflecting the fact that they demonstrate a wide variety of biological activities.

Email: Copyright 2014 Scientific Academic Publishing. There are hydroxamates with reported anti-HIV activity such as the hydroxyurea which acts as inhibitors of cellular enzyme ribonucleoside diphosphate reductase. 1 Hydroxamates have high affinity for ferric ions that nature has evolved families of hydroxamic acids to function as no N-binding compounds siderophores in bacteria.

The method has been success fully applied to enantiomerically pure esters without loss of stereochemical integrity. 1-Propanephosphonic Acid Cyclic Anhydride T3P Promoted Synthesis of Hydroxamic Acid1-Propanephosphonic acid cyclic anhydride T3P promotes the synthesis of hydroxamic acids from carboxylic acids.

34 Application of ultra-sonication was showed to accelerate this conversion.

This process increases the amount of RNA present in the cell and their respective encoded proteins. Synthesis of Trichostatin A Trichostatin A was the first naturally occurring HDI to be discovered. It causes an increase in acetylated histones in a variety of mammalian tumor cell line.

Alcohol 26 was treated with 2-methoxy propene and pyridinium p-toluenesulfonate PPTS to generate protected diol 27. To achieve this, the ester 0.5 M in methanol and hydroxyl amine 10 eq was reacted in the presence of sodium methoxide 1 eq. Following an optimization studies, they found that at 70 and 30 min, highest yield of the hydroxamate was obtained with high purity. Microware Activated Hydroxamic Acid Synthesis Massaro et al 33 has shown that the reaction of esters with hydroxylamine in the presence of a base under microwave activation provides hydroxamic acids in good yield and high purity. The syntheses of various classes of hydroxamates and their mode of biological applications have been reviewed. 4 Much of their activities are due to their chelating properties with metal ions, especially with transition metals, hence constituting a very important class of chelating agents with versatile biological activities. The broad biological activities of hydroxamates and the need to improve on their synthetic routes informed the review of their synthesis and biological applications. 5, 6 A number of synthetic routes are available for the preparation of hydroxamic acids, 7-12 but some are tedious, time consuming and costly as well. Colombo, An improved synthesis of the HDAC inhibitorn trichostatin A, Master s Theses and Doctoral Dissertations, Eastern Michigan University, 2009, 1-2.