Antimictobial Activities And Structure-activity Relationships Of 2-aryl-3, 4-dihydroisoquinolines Bromides

Isoquinoline quaternary ammonium salt own various biological activities, such as antitumor, antimicrobial, antioxidation and so on. And many studies have proved that the structure of the polar bond C=N~+ is active-position.However, the further research has been limited by the lack of species in plant and the sensitivity of chemical pro-perties.There is a effective way - take the structure of these compounds as templates,to solve this negative.Our lab has designed and synthesized 29 compounds-2-aryl-3,4-dihydroisoquinoline bromides (ADHIQs),based on the structure of the structure of the isoquinoline quaternary ammonium salt and made research on its acaricidal activity .In order to provide more theoretical basis for the future research of .biomimetic synthesis, this paper is to make a further study on antimicrobial activity and structure-activity relationships of ADHIQs.The preliminary analysis of the antibacterial activity and structure-activity relationships are based on the three aspects result:plant pathogenic fungi,bacteria and multidrug-resistant Escherichia coli .1 the result of antifungi exhibits that 29 ADHIQs have different inhibition against mycelial growth of 12 plant pathogenic fungis at the conceration of 50mg/L .The inhibition rate of four compounds (2Cl, 4Cl, 2F and 4F) is more than 60%. The half maximal effective conceration of four compounds against Curvularia is 8.05 ~ 13.05 mg/L.Seven modified ADHIQs result show that 1-PrO can improve the activity .2. The result of MIC of bacteriostatic test show that 2I is best in against E. coli, the molar concentration of MIC is 6.039μmol/L, the mass concentration is 2.5mg/L; and 4I is best when used to against Staphylococcus aureus ,the mass concentration is 1.25mg/L. 3. The result of multidrug-resistant Escherichia coli . 4F and 2Me are better, MIC is 8 mg/L at mass concentration,which expressed that the introduction of substituents of 2′-Me and 4′-F would improve antibacterial activity.