Synthesis, antimicrobial, DNA cleavage and antioxidant activities of tricyclic sultams derived from saccharin

摘要

Abstract Two series of fused tricyclic sultams (carboxylates, 3a, b and 5a, f, g and anilides 5b-e) were synthesized from saccharin and their chemical structures were confirmed by spectroscopic tools. Then, their antibacterial activities and MIC were evaluated against two strains of gram positive and gram-negative bacteria. The MIC values of the tested compounds are in the of range 8–33?μg/ml. In addition, their DNA cleavage ability, binding affinity and their anticancer activities against hepatic cancer cell were tested. And their antioxidant activities were also measured. Four carboxylate derivatives ( 3a, 5a, 5f and 5g) and one anilide ( 5d ) of the tested compounds proved to be the highest activity all over the study. Highlights ? Two series of fused tricyclic sultams have been synthesized from saccharin in excellent yield. ? Four derivatives of the tested compounds showed very good antimicrobial activity. ? Three derivatives showed significant antioxidant activity compared to the reference compound. ? One of the tested compounds showed a significant anticancer activity against hepatic cancer cell.