Studies On The Synthesis And Anti-bactericidal Activity Of New 2-Substituted Aryloxy Acetyl Hydrazono-1, 3-dithocyclopentane Derivatives

The heterocyclic derivatives have the extensive application and the research values in the medicine and agrochemical. Some research works have showed "2-substituted hydrazono-1, 3-dithocyclopentane"derivatives have good bioactivity. It is an important precursor for us to obtain more new compounds, which have higher effect, wilder application, better selectivity and lower toxicity. This article concentrates on the synthesis and anti-bactericidal activities of the new 2-Substituted aryloxy acetyl hydrazono -1, 3-dithiocyclopentan derivatives. Quantitative Structure-Activity Relationships (QSAR) plays an important role in drug's discovery, because it can predict compound's bioactivity and helps us to discover the relationship of the pharmacal effect and the target molecules (TM) structure. On the basis of Free-Wilson model, two kinds of target molecules owning potential bioactivity are designed. The following innovated results were achieved: (1) Six new 2-substituted aryloxy acetyl hydrazono-1, 3-dithocyclopentane have been designed and synthesized. All of them are reported for the first time and their structures have been confirmed by IR, 1H NMR, MS and elemental analysis. (2) The other kind of 2-Substituted diphenoxyl acetyl hydrazono-1, 3-dithocyclopentane derivatives have been synthesized via arylation the biphenyl acetyl chlorine and 2-hydrazono-1,3-dithocyclopentane. Their structures have been confirmed by IR, 1H NMR, MS and elemental analysis. (3) The anti-bactericidal test was carried out. We chosen five targets and seven kinds of bacterium in this test. Studied on the test and we found the following results: a). all of the tested compounds have good anti-bacteria activity. The targets have antimicrobial activity on S. aureus, E. coli, S. Ligneres, P.Vulgaris and D.cata, et al. b). The target which contains fluoro-substitution has the best anti-bacteria activity among all this targets. (4) All the target molecules have more extensive anti-bactericidal activity than tricyclazole and thiophanate-methyl (on sale), which are anti-bacteria agents widely used. The thorough researches in future can provide probably the practical good anti-bacteria compounds. These studies give a good basis to expand the researches and applications of the 2-Substituted aryloxy acetyl hydrazono-1, 3-dithocyclopentane and the related derivatives.