Studies on anticoccidial agents. 12. Synthesis and anticoccidial activity of methyl-2(6)-nitro- and -3(5)-nitropyridinecarboxamides

• Published in: Journal of medicinal chemistry Vol. 21; no. 2; pp. 194 - 199
• Main Authors: Morisawa, Yasuhiro, Kataoka, Mitsuru, Sakamoto, Toshiaki, Nagahori, Hitoshi, Kitano, Noritoshi, Kusano, Kenichi
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 01.02.1978
• Subjects: Coccidiostats - chemical synthesis; Eimeria - drug effects; Isonicotinic Acids - chemical synthesis; Isonicotinic Acids - pharmacology; Nicotinic Acids - chemical synthesis; Nicotinic Acids - pharmacology; Picolinic Acids - chemical synthesis; Picolinic Acids - pharmacology; Structure-Activity Relationship
• ISSN: 0022-2623; 1520-4804
• DOI: 10.1021/jm00200a010

A number of methyl-2- and 3-nitropyridinecarboxamides have been synthesized. It has been established that the presence of at least one hydrogen atom, adjacent to the NO2 function, is important for anticoccidial activity and introduction of a methyl group to the adjacent position of the CONH2 function sometimes confers enhanced activity. Among the compounds herein, 5- and 6-methyl-2-nitropyridine-4-carboxamides possess optimal anticoccidial activity, being as potent as the parent compound.