Nicotinic acid prodrugs

Preparation of the first of these antiinflammatory prodrugs starts with the displacement of halogen on bromophthal ide 2 by the anion of the nicotinic acid derivative 1. Reaction of the intermediate 3 with aniline 4 leads to formation of talniflumate (5). ... 

A. Salvi, P. A. Carrupt, J. M. Mayer, B. Testa, Esterase-Like Activity of Human Serum Albumin toward Prodrug Esters of Nicotinic Acid , Drug Metab. Dispos. 1997, 25, 395-398. 

Table 8.5. Chemical and Enzymatic Hydrolysis of Ester Prodrugs of Nicotinic Acid (8.33) at... 

A simple example of bioprecursor prodrug is found in dexpanthenol and 3-pyridine-methanol (Fig. 33.26). These primary alcohols are the reduced forms of the vitaminic factors pantothenic acid and nicotinic acid, respectively. Dexpanthenol has the advantage over the parent drug of being more stable, especially towards racemization. 

Tashtoush BM, Bennamani AN, and Al-Taani BM. (2013). Preparation and characterization of microemulsion formulations of nicotinic acid and its prodrugs for transdermal delivery. Pharmaceutical Development and Technology, 18, 834-843. 

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