Synthesis And Antibacterial Activity Of Novel Porphyrin-1,4-dihydropyridine Compounds

With the widespread use or unreasonable use of broad-spectrum antibiotics, drug resistance problem is more serious, which threat to human health. Thus, searching high efficiency, low toxicity anti-microbial agents becomes imminent. Due to the non-specificity and efficiency of Photodynamic Antimicrobial Chemotherapy, it is concerned by making pathogen hard to have a drug resistance. The efficacy of Photodynamic antimicrobial chemotherapy depends on photosensitizer. This paper focuses on the synthesis of new porphyrin photosensitizer and the antibacterial activity of target molecules. For the purpose of Synthesis new antimicrobial drugs, we designed and synthesized novel 22 porphyrin -1,4 - dihydropyridine compounds, and its antimicrobial activity were discussed. Details are as follows:1. Designed and synthesized 22 kinds of porphyrin 1, 4 - dihydropyridines antibiotics, all compounds have not been reported. We confirmed their structure by the necessary structural characterization.2. According to two important ways of drug design principles: The design of analogues and Mosaic theory. Using the molecular structure characteristics of monohydroxyporphyrin and 1,4 - dihydropyridine , We connected them simply as the dibromoalkanes for the bridge. The method is simple, raw materials easily be obtained, yield is higher and post-processing is more convenient. Provide a basis for the synthesis of new drugs.3. Using training method of beef extract medium, we calculate the inhibition of compounds on Staphylococcus aureus and Escherichia coli by measuring the OD value of experimental and control group .We found that compounds 30b, 30d,31b,32c have good inhibition effects on Staphylococcus aureus at a concentration of 2.0×10^-4mol / L, the Inhibitory rate can reach to 90%. And compound 29e has favorable restraint effect on Escherichia coli at the level of 2.0×10^-4mol/L, the inhibitory rate up to 94%.