Document Report Card

ID: ALA1121588

Journal: J Med Chem

Title: Studies on anticoccidial agents. 13. Synthesis and anticoccidial activity of nitropyridine-2- and -3-sulfonamides and derivatives.

Authors: Morisawa Y, Kataoka M, Nagahori H, Sakamoto T, Kitano N, Kusano K, Sato K.

Abstract: Eight nitropyridinesulfonamides and pyridinesulfonamide N-oxides as their bioisosteres were prepared and evaluated for anticoccidial activity. Of these compounds, 2-, 4- and 5-nitropyridine-3-sulfonamides and pyridine-2- and -3-sulfonamide N-oxides were found to be active against Eimeria tenella. Thus, the relative positions, ortho or meta, of the substituents in nitropyridine-3-sulfonamides and pyridinesulfonamide N-oxides are important for anticoccidial activity. N-Substituted analogues of 5-nitropyridine-3-sulfonamide were also prepared and optimal anticoccidial activity was attained with the sulfonamide and its lower N-alkyl derivatives. The mode of action of 5-nitropyridine-3-sulfonamide was examined and found to be active in the sporozoite and the first schizogony stages.

CiteXplore: 7452692

DOI: 10.1021/jm00186a017