Synthesis And Analysis Of Several Derivatives Of Tyrosine For Treatment Of Diabete Ⅱ

Diabetes is a chronic disease that is associated with a high degree of morbidity and mortality. Its primary endangerment is chronic syndrome which leads to pathological changes of some apparatus due to hypertension and metabolizability turbulence which are induced by insulin resistance. This disease can also lead to lunacy, nephropathy, retinopathy, high plasma triglycerides and other disease. Some new antidiabetic drugs were invented with high efficiency and obvious toxicity.The molecular mechanism of thiazolidinedione (TZD) is activation of peroxisome proliferator-activator receptor gamma (PPARγ). The PPARγ agonist TZD class of antidiabetics has been shown to improve insulin resistance and reduces hypertension. In this theses, it's reported that some novel antidiabetics compounds with higher activity of both PPARαand PPARγreceptors than rosiglitazone at the same concentration . These compounds can improve insulin sensitivity and effectively decreases free fatty acids and triglycerides. The main content is followed: 1. Synthesis and analysis of 2-[(1-methyl-2-benzoyl)-vinylamino]-3-{[4-(2-carbazol-9-yl)-ethoxyl] phenyl} propionic acid and 2-[(2-benzoyl)-phenylamino]-3-{[4-(2-carbazol-9-yl)-ethoxyl] phenyl}propionic acid. The former is unstable in weak acidic medium, the latter which has been protected in patent requires to be modified and synthesis the followed compounds.2. Synthesis and analysis of 2-[2-(4-fluorobenzoyl) phenylamino]-3-[4-(2-carbazol-9-yl-ethoxy)-phenyl]-propionic acid and 2-{1-[2-(4-chloro (hydrogen) benzoyl)]-cyclohexanamino}-3-[4-(2-carbazol-9-yl-ethoxy)-phenyl]-propionic acid. Two series of were synthesized due to hydrogenolysis during dehydrogenation in the reaction of raw material. The former is very stable while the latter is quite unstable and to get highly in pure.3. Synthesis and analysis of 2-[2-(4-substituted benzoyl) phenylamino]-3-{[4-(2-carbazol-9-yl)-ethoxy]-phenyl}-propionic acid. Structures of synthesized products were affirmed by ultraviolet, infrared, nuclear magnetic resonance spectroscopies and mass spectrometry. Some target compounds possess high PPARγactivity and are worthy to research and develop further.