Morisawa Y, Kataoka M, Sakamoto T, Nagahori H, Kitano N, Kusano K
J Med Chem. 1978 Feb;21(2):194-9. 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.
已经合成了多种甲基 -2- 和 3- 硝基吡啶甲酰胺。已经确定,与 NO2 官能团相邻至少有一个氢原子对于抗球虫活性很重要,并且在 CONH2 官能团的相邻位置引入甲基有时会赋予增强的活性。在本文所述的化合物中,5- 和 6- 甲基 -2- 硝基吡啶 -4- 甲酰胺具有最佳的抗球虫活性,与母体化合物一样有效。