Synthesis And Anti-microbial Activity Of Vitamin B₃Derivatives

Microbial infection causes some common disease. In recent years, the wide and excess quantity use of antibiotic, antineoplastic, immune suppressants has resulted in the weakening of body’s defenses capability, and the substantial increasing of incidences caused by microorganisms. At the same time, a lot of use of anti-microbic drugs for a long time has resulted resistance increasing against anti-microbic drugs. Therefore, there is an urgent need to develop a new generation of drugs with broad-spectrum activity, low toxicity, and high efficiencity against microorganisms.Pyridine and its derivatives are widely distributed in nature, with the deepening of people research, pyridine and its derivatives are used in the pharmaceutical and chemical production. And some pyridine derivatives have a better biological activity, low toxicity, high selectivity, and excellent performance in anti-microbic.2-methylpyridine can be used to synthesize chlorpheniramine, long-acting sulfonamides. local anesthetics:3-methylpyridine can be used for synthesizing of nicotinic acid, nicotinamide. vitamin B. cardiac drugs and other drugs;4-methylpyridine’ s system is used in the manufacture of isoniazid. it was widely used in anti-tuberculosis. Nicotinic acid derivatives with good biological activity in the pharmaceutical industry, extensive research and application.This thesis is based on the status of the research and development above. starting from2,6-dimethy1-3,5-dimethyl ethyl pyridine synthesis of three2,6-dimethy1-3,5-bromo-pyridine dicarboxylate derivatives design by bromination reaction2,6-dimethy1-3,5-dimethyl ethyl pyridine has a number of α-H. so that the reaction produces a large number of multi-brominated accessory substance, affecting the target the product yield. The experiment from the order of addition, the feeding mode, reaction time and other aspects of the reaction is optimized to find the optimum reaction conditions. Subsequently brominated derivatives of2,6-dimethy1-3,5-dimethyl ethyl pyridine are used for ammonolysis. etherification and hydrolysis. and these methods are analyzed and compared, to find the best synthetic methods and conditions. The ultimate synthesis include14new compounds.In this paper, the filter paper method and punch method were used for testing invitro anti-microbic of the substances. We can see from the experimental results of the biological activity for selected13compounds, in addition to the zy-01, zy-12, zy-11, zy-12have good activity, the effect of anti-microbicl of other substances is extremely weak. zy-01and zy-02are good at antibacterial for several bacteria, zy-11and zy-12have certain inhibitory effect on bacteria and fungi.