The preparation of some 4-substituted nicotinic acids and nicotinamides

Abstract

Nicotinamide adenine dinucleotide (NAD) analogues in which the 4-position of the pyridine ring carries a substituent are potential inhibitors of the glycolytic process by which many cancer cells derive an appreciable proportion of their energy requirements. Such analogues should be produced in vivo by the administration of 4-substituted nicotinic acid derivatives.

The preparation of the following derivatives is now described: 4-hydroxy-, 4-methoxy-, 4-butoxy-, 4-(2-hydroxyethylthio)-, 4-S-cysteinyl-, 4-amino-, 4-anilino-, and 4-benzylamino-nicotinic acid and -nicotinamide. 4-Ethoxy- and 4-(2-bromoethylthio)-nicotinic acid and 4-benzylthionicotinamide were also obtained.

A preliminary report on the biological activity of some of the derivatives is given.