Wednesday, July 27, 2011

Antagonists of Pantothenic Acid

Pantothenic Acid Antagonists 
Pantoyltaurine has been studied extensively as an antimetabolite of pantothenic acid. 
Inclusion of this compound in the diet of animals leads to deficiency symptoms. Twenty-five, derivatives of this compound were prepared and studied for inhibitory activity. Another antagonist that has been studied in various species is co-methyl pantothenic acid. This compound interferes with the formation of CoA and produces typical deficiency symptoms in animals. 
This compound was used to produce human pantothenic acid deficiency discussed previously. Antagonists of pantothenic acid probably all act by inhibiting normal functions of CoA. It is reasonable to suppose that of the many functions of this coenzyme, some would be affected to a greater extent than others, due to different degrees of coenzyme-apoenzyme and enzyme­substrate affinity, etc. 
Dietrich and Shapiro showed that ro-methylpantathine markedly inhibited sulfanilamide acetylation at concentrations which were ineffective against citrate formation in pigeon liver homogenates. On the other hand, bis (pantoylaminoethyl) disulfide was found to inhibit citrate formation at concentrations which did not affect sulfanilamide acetylation. The action of 6­mercaptopurine in blocking nuclear mitosis in animals can be reversed by administration of pantothenic acid or coenzyme A.