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With the widespread use of antimicrobial drugs , bacterial resistance has developed into a serious public health problem . The emergence of resistant strains , making the otherwise easy to deal with the infection becomes clinically difficult to treat , constitute a great threat to the clinical anti-infection treatment , caused global concern . Solve the problem of bacterial resistance to antibiotics , research and development of new antibacterial drugs without delay . Task Force preliminary studies found a resistance to multi - drug-resistant Gram- positive bacteria compound A01 , in order to enhance the antibacterial activity of the A01 , to broad-spectrum antimicrobial spectrum more characteristics , we designed several series of aromatic vinyl imidazole class structure , were synthesized 53 derivatives ( A02 -54 ) , 31 of which contain 4 - substituted imidazole structure derivatives as novel structural compounds (A21, A23-24 and A27- 54) . All designed and synthesized 53 derivatives , select 7 clinical resistant strains (including three kinds of G bacteria and four kinds of G-bacteria ) , carried out in vitro antibacterial activity test . Found a total of 31 derivatives of three kinds of drug-resistant G bacteria have a strong antibacterial activity ( three MIC ≤ 32μg/mL ) , three MIC lt; a 10μg/mL the active compounds 20 , the three MIC ≤ 2μg/mL of the active compound 12 (A28, A30-A32, A34, A37, A39-A41, A44, A45, A49), the most active compound of the A30, its three MIC respectively 1,1,0.5 gg / mL. It is worth noting that the derivatives A12 showed a certain degree of broad - spectrum antibacterial properties , especially considering the A12 extremely simple molecular structure, molecular weight of only 200, corresponding to the molecular size of a fragment , it has a strong transformation space , worthy of further study . Based results of susceptibility active , summarize the structure-activity relationship of substituted aryl vinyl imidazole compounds , provides useful information for further design and development of new broad-spectrum anti- drug-resistant drugs .
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