Design, Synthesis, Characterization and Biological Evaluation of Benzothiazole Fused Guanidinopropionic Ester Derivatives.

A novel series of Benzothiazole fused Guanidinopropionic ester derivatives have been synthesized and characterized by FTIR, 1HNMR and mass spectral analysis. All the compounds were evaluated for their Aldose reductase (enzyme inhibition assay) and DPPH free radical (Scavenging assay) further more evaluated for antimicrobial activities (Disc diffusion and MIC method) against some pathogenic bacteria and fungi. Results revealed that, compound BC 12d exhibited promising AR inhibitory (80% inhibition, 10μm), free radical scavenging (95% inhibition) and antimicrobial activities (MIC 12.5-6.25μg\ml) at varied concentrations. The most active compound BC 12d has been docked into the crystal structure of Aldose reductase. Docking results indicate hydrogen bond interactions (2.25 Å) between the carbonyl group of ester in compound and the catalytic amino acid residues Arg 265 and Ser 261