The Synthesis And Bioactivity Of Novel Triazolopyrimidine Derivatives(Ⅲ)

The research progress of triazolopyrimidine derivatives and 3-substituted - 4-amino-5-mercapto-l,2,4-triazole derivatives were reviewed in this paper. According to the principle of combination of bioactive sub-structure, twenty-eight new diheterocyclic compounds containing l,2,4-triazolo[l,5-a] pyrimidine and 1,2,4-triazole moieties were designed and synthesized, whose structure were confirmed by !HNMR, MS and I3CNMR spectroscopy. The title compounds can be divided into two series accordding to their structures categories,shown as following: (1 )3-(5,7-dimethyl-s-triazolo[ 1,5-a]pyrimidine-2-thiomethylene)-4-arylideneamino-5-mercapto-s-triazole (I).(2)3-(5,7-dimethyl-s-triazolo[l ,5-a]pyrimidine-2-thiomethylene)-4-amino-1,2,4-tria zole-5-thio-ether (II).The biological activity of all compounds synthesized were tested priliminarily. The results showed that compounds I displayed fungicidal activity against A.mali to some extent, and some of II showed good fundicidal activity against C.beticola. The biological activity may be strengthened by the structure containing phenyl. Especially, I-01, 11-01, 11-02, II -03, II-06, and II-08 show goodactivity for C.beticola, furthermore, II -01 shows good activity for G.saubinetii.In addition, compounds I showed stimulative effect for Rape stem at the concentration of lOOppm. On the other hand, compounds II showed good herbicidal activity against the root of Barnyard grail and stimulated the growth of its stem. In addition, most tested compounds (I) indicated good activity for the growth regulation of wheat bud, especially I-10 at the the concentration of lOOppm.