Based On The Synthesis, Characterization And Biological Activity Test Of Heme-anti-schistosomiasis Compounds

Schistosoma is one of the parasites, and it is also known as schistosome for androgyny. It lives in the host's vein.Schistosomiasis can cause schistosomiasis and it is the second world's serious parasitic disease(first malaria), especially common for children in developing countries.Carbazole and its derivatives are one of the important aromatic nitrogen containing heterocyclic compounds. Since the molecules contain large conjugated system and relatively strong in molecular electron transfer. This special rigid fused ring structure, which the carbazole compounds will highlight show many special properties and biological activity. The more important is that these carbazole compounds are easier modification on the structure, so it is very convenient to introduce other kinds of functional groups in the carbazole ring. Benzene and naphthalene pyridine compounds not only have rigid plane of nitrogen heterocyclic structure, but also connected with benzene ring. The electron density increases greatly and have more lively reactivity. It can introduce a variety of different groups on the benzene ring and nalidixic forming a series of derivatives. These derivatives have good biological activities. Because carbazole compounds,benzene and nalidixic compounds have active role on schistosomiasis, so these design and synthesis two series of compounds.(1) These have synthesized 30 carbazole- amino alcohols compound(e-1~e-30).It tested these compounds' composition and structure through MS, NMR and methods of melting point determination. These proved that this kind of compounds have been successfully synthesized. It tested these compounds' activity of its resistance to schistosomiasis by in vitro simulation experiment of schistosomiasis, schistosomiasis adult in vitro experiments and mice experiment preliminary biological activity test. More importantly, we find carbazole amino alcohols compounds e-11 and e-29 stayon schistosomiasis better inhibitory through three biological activity test experiment. These show broad prospects and potential application value in resistance to schistosomiasis in drug development.(2) These have synthesized 13 Benzene and naphthalene pyridine compounds(i-1 ~ i-13).It tested these compounds' composition and structure through MS,NMR and methods of melting point determination. These proved that this kind of compounds have been successfully synthesized. It tested these compounds' activity of its resistance to schistosomiasis by in vitro simulation experiment of schistosomiasis, schistosomiasis adult in vitro experiments and mice experiment preliminary biological activity test. More importantly, we find Benzene and naphthalene pyridine compounds i-1?i-2?i-4 and i-9 stay on schistosomiasis better inhibitory through three biological activity test experiment. These show broad prospects and potential application value in resistance to schistosomiasis in drug development.