Abstract:
A series of N-(
α-eleostearic acyl) triazole compounds derived from
α-eleostearic acid were synthesized: N-(
α-eleostearic acyl)-3, 5-dibromo-1, 2, 4-triazole(
3a), N-(
α-eleostearic acyl)-1, 2, 4-triazole(
3b), N-(
α-eleostearic acyl)-3-sulfhydryl-1, 2, 4-triazole(
3c), N-(
α-eleostearic acyl)-5-nitro-1, 2, 4-triazole(
3d), N-(
α-eleostearic acyl)-1, 2, 3-benzotriazole(
3e), 3-(
α-eleostearic acyl)-1, 2, 4-triazole(
3f), 4-(
α-eleostearic acyl)-1, 2, 4-triazole(
3g). The products were confirmed by FT-IR,
1H NMR,
13C NMR and MS. The results of biological activity experiments showed that compound
3a and
3e had inhibitory effect on hepatocarcinoma cells Hep G2, rectal carcinoma cells DLD-1 and breast cancer cells MCF-7. The 50% inhibition concentration(IC
50) of compound
3d on MCF-7 was 25.12 μmol/L, which was better than the IC
50 of 5-fluorouracil(5-Fu). All compounds had good inhibitory activity against
Candida albicans, and inhibitory activities on against
Escherichia coli and
Staphylococcus aureus were not significant. The IC
50 of compound
3e against
Candida albicans was 22.96 mg/L, which was similar to 5-flucytosine and indicated that it had the potential of drug development.