Design, synthesis and biological evaluation of novel 2-methylpyrimidine-4-ylamine derivatives as inhibitors of Escherichia coli pyruvate dehydrogenase complex E1

J He, L Feng, J Li, R Tao, F Wang, X Liao, Q Sun…

Index: He, Junbo; Feng, Lingling; Li, Jing; Tao, Ruijuan; Wang, Fang; Liao, Xun; Sun, Qiushuang; Long, Qingwu; Ren, Yanliang; Wan, Jian; He, Hongwu Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 5 p. 1665 - 1670

Full Text: HTML

Citation Number: 19

Abstract

As potential inhibitors of Escherichia coli pyruvate dehydrogenase complex E1 (PDHc E1), a series of novel 2-methylpyrimidine-4-ylamine derivatives were designed based on the structure of the active site of PDHc E1 and synthesized using 'click chemistry'. Their inhibitory activity in vitro against PDHc E1 and fungicidal activity were examined. Some of these compounds such as 3g, 3l, 3n, 3o, and 5b demonstrated to be effective inhibitors of ...