Design, Synthesis and DNA Cleavage Studies of benzofuran-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine derivatives

Abstract

Purpose: Benzofuran is a significant heterocyclic compound, constituting the structural context of bioorganic and medicinal noteworthy organic compounds.  Therefore, in this study synthesis and evaluation of DNA cleavage activity of benzofuran fused thiadiazine derivatives (IVa–h) was discussed.

Methodology: Benzofuran fused thiadiazine derivatives were synthesized by the fusion of commercially available benzofuran-2-carboxylic acid (I) with thiocarbohydrazide (II) followed by condensation reaction with different phenacyl bromides (a-h). The synthesized compounds were characterized by phisico-chemical spectral analysis such as melting point, elemental analysis, FT-IR, ¹³C NMR, ¹H NMR, and mass spectroscopy studies. The DNA cleavage efficacy was evaluated using agarose gel electrophoresis.

Analysis/Results: The DNA cleavage studies of all synthesized compounds (IVa-h) were photolyzed at 365 nm, at 50µM concentration in the presence of pUC19 DNA. The study shows that the compounds IVa and IVb showed a more intense streak, indicating better activity than that of other compounds.

Originality/Value: Synthesis and DNA cleavage evaluation of benzofuran fused thiadiazine derivatives were not explored. DNA cleavage studies, it is observed that some of the synthesized derivatives have exhibited better DNA cleavage activity. The obtained results recommend that these classes of compounds can be considered as new templates for further structural optimization to achieve better biological drug development.

Type of Paper: Experimental.