Abstract: 3-Aliphatic-1,2,4-triazole derivatives 1a~1f were synthesized through the reaction of six kinds of fatty acids with diaminothiourea, in which compounds 1e and 1f were first synthesized. In the presence of phosphorus oxychloride, compounds 1a~1f reacted with 4-pyridine carboxylic acid and 2,6-pyridine dicarboxylic acid, respectively. The 12 kinds of aliphatic triazoles, thiadiazoles 2a~2f and 3a~3f were synthesized in high yields for the first time. In order to study the influence of 3-aliphatic group and pyridine, compounds 5, 6, 7a~7c and 8a~8c without pyridine units were also synthesized. The target compounds were well characterized by IR, 1H NMR and HRMS. In the biotic screening test, the inhibitory properties of Cdc25B and PTP1B were explored. The results show that compounds 3b, 3d, 3e and 3f have good inhibition activity against Cdc25B with IC50 values of (1.12±0.27), (2.72±1.07), (0.72±0.05) and (4.97±0.93) mg/L, respectively; compounds 2b, 3d, and 5 exhibit higher inhibition activity against PTP1B with IC50 values of (0.98±0.13), (1.33±0.11), (2.18±0.20) mg/L, respectively.

Key words: aliphatic-triazole, pyridine unit, biotic screening test, Cdc25B,PTP1B inhibitor