The Studies On Synthesis And Bioactivity Of Multisubatituted Pyrrolic Thiosemicarbazone

Thiosemicarbazones with good biological activity and strong coordination ability are a class of anti-inflammatory, bactericidal, antiviral, antitumor, which has been still one of the hot topics of medicinal chemistry. Multisubstituted pyrrole and its derivatives with various biological activities are important pentatomic heterocyclic compounds. As an important intermediate of fine chemical products, pyrrole and its derivatives are widely used in pesticides, medicine, food and polymers material fields.In this paper,1,2,3,5-tetrasubstituted pyrrole derivatives were introduced into the substituted thiosemicarbazides according to the principle of combination of bioactice substructures, thus synthesizing a series of multi substituted pyrrolic thiosemicarbazones. The contents are as follows:1. Based on extensive relevant literatures, this paper separately expounded the synthetic method and application progress of thiosemicarbazones and multi substituted pyrrole compounds.2. Four1,2,3,5-tetrasubstituted pyrrole derivatives were synthesized by Paal-Knorr reaction using microwave radiation method. N4-substituted thiosemicarbazides and ethane-1,2-dithiosemicarbazide were prepared using CS2, hydrazine hydrate and primary amines as raw materials, thus synthesizing32multi substituted pyrrolic thiosemicarbazones. The conditions such as the solvent, material ratio and the temperature were optimized by experiments.3. The structures of intermediates and the target compounds were established by1H NMR, MS and element analysis data.4. The antibacterial activities of the target compounds in vitro were studied by Filter Paper Method and Dilution Method. Escherichia coli and Staphylococcus aureus were the test models. The results showed that the target compounds against Escherichia coli and Staphylococcus aureus has certain antibacterial activity.5. The antitumor activities of the multi substituted pyrrolic thiosemicarbazones in vitro were studied with SRB Method and MTT Method. The synthesized compounds possessed varying antitumor activity.6. The structure-activity relationship of the series of compounds was preliminarily discussed based on the biological test datas.