Synthesis and Pharmacological Properties of Glutamic Acid Amides: A Review

personАвтори: Al. Zlatkov, G.Stavrakov, J. Tencheva, P. Peikov, Y. Voynikov


The present study is a review of known methods and strategies for synthesis of amides with emphasis on glutamic acid (GA) amides. Amides can be prepared by activation of the corresponding carboxylic acids to acyl halides (chlorides and fluorides), acyl azides, anhydrides or esters using various coupling reagents like carbodiimides (DCC, EDC, DIC, etc.), organophosphorous reagents (BOP, PyBOP, DPPA, etc.) or aminium reagents (HOBt, HBTU, TBTU, etc.). After activation subsequent reaction with the desired amine follows, to produce the amide.  Discussed in this review are also the pharmacological properties of GA amides as prodrugs. These prodrugs exhibit generally enhanced cell permeability, stability and bioavailability combined with good safety. Prodrugs with GA may be beneficial as a substantially improved oral administration form and warrant future research toward development of new drugs.

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