吡啶衍生物合成及抗幽门螺杆菌活性研究

Synthesis and Anti-Helicobacter Pylori Activity of Pyridine Derivatives

合成了系列吡啶衍生物,并对其进行抗幽门螺杆菌(Helicobacter pylori,HP)作用研究,以得到较高活性的先导化合物。以2-氯甲基-3-甲基-4-甲氧基吡啶盐酸盐为原料,通过亲核取代、间氯过氧苯甲酸(m-CPBA)氧化合成了系列吡啶衍生物;采用琼脂扩散法,以阿莫西林为阳性对照,进行了初步体外抗幽门螺杆菌(Anti-Helicobacter pylori)活性评价。成功合成了2a^2c、3a^3c、4a、5a、6a^6c十一个吡啶衍生物,并经过MS、~1H NMR和^(13)CNMR结构确证,发现化合物2a、6a均有良好活性。由此发现了新型的具有抗幽门螺杆菌作用的吡啶类先导化合物。

We compounded a series of pyridine derivatives and evaluatea ItS activity oI anu- Helicobacter pylori to get lead compounds with higher activity. The target compounds were synthesized through nucleophilic substitution, oxidation by m-CPBA using 2-chloromethyl-4-methoxy-3- methylpyridine hydrochloride as starting material, and evaluated anti-Helicobacter pylori activity of pyridine derivatives by the agar diffusion method and amoxicillin as positive control. The target compounds were successfully synthesized and verified by ~3 CNMR, 1 H NMR and MS spectra, which included 2a ~2c, 3a ~3c, 4a, 5a, 6a ~6c, etc. llcompouds al~ er, and then found that 2a and6a exhibited comparable efficacy to amoxicillin. A new family of anti-Helicobacter pylori activity of pyridine derivatives is disclosed.