Synthesis And Antimicrobial Activity Of Novel Triazole Derivatives

Infectious diseases have increased in frequency and severity for the past few years as a result that not only broad-spectrum antibiotics,corticosteroids and immune inhibitors,but also HIV,organ transplantation and intervention techniques are widely used.In particular,one of the major problems is occurrence of antibiotics resistance.It's a challenge for researchers to find new candidates with antimicrobial activities.Triazole compounds are those ones,for better biological activities,high efficiency,low toxicity,wide antimicrobial spectrum,and stereoselectivity characteristics Thus,triazole compounds are good drugs for the treatments,such as antifungal,antibacterial,antituberculosis,anticancer,antivirus and anti-inflammatory.In this study,we extensively investigated the structure,mechanism and research progress of 1,2,4-triazole compounds.We designed and synthesized series triazole compounds with the 1,2,4-triazole ring as the efficacy groups.In addition,we prepared two serials of 1,2,4-triazole compounds by two roads.To the best of our knowledge,nine of them are reported for the first time.1)1,3-dichlorobenzene was used as raw material,and substituted by chloroacetyl chloride.The products were following substituted by 1,2,4-triazole,and then ware reducted by sodium borohydride.Finally,9 phenethyl alcohol triazole compounds were synthesized,purified and characterized.2)Phenyl amines compounds were reacted with chloroacetyl chloride and substituted by 1,2,4-triazole.Then 6 acetanilide triazole compounds were obtained,purified and characterized.All products were characterized by 1HNMR,IR,MS,EA and their physical and chemical properties were obtained.Then,antibacterial and antifungal activities of these compounds in vitro were determined by antibacterial sensitivity experiment method which is recommended by National Committee for Clinical Laboratory Standards(NCCLS).The results suggest that compounds 1(a-i)display better activities against fungi and gram-positive bacteria than compounds 2(a-f).The mechanism of these triazole derivatives is proposed.Finally,their structure-activity relationships(SAR)are carried on the preliminary analysis.