Green synthesis, biological and spectroscopic study on the interaction of multi-component Mannich bases of imidazo[2,1- b]benzothiazoles with human serum albumin

摘要

AbstractA series of Mannich bases of imidazo[2, l-b]benzothiazoles were prepared through one-pot multi-component reaction in the presence of water as an eco-friendly solvent. All the synthesized compounds were confirmed from IR,1HNMR,13CNMR, and Mass spectroscopy. Evaluation of in vitro anti-inflammatory and anti-microbial activities of all the synthesized derivatives was further accomplished. These results clearly displayed that compound6dexhibited outstanding anti-inflammatory activity with a percentage inhibition of 70.23% by membrane stabilization method whereas 67.54% at 100μgmL?1by the albumin denaturation method, which is comparable to the standard Diclofenac. Further screening against five fungal species (C. albicansATCC 76615,C. mycoderma, C. utilis,A. flavus, andB. yeast) along with four gram positive (Methicillin-resistantS. aureusN315 (MRSA),Staphylococcus aureusATCC 6538,Bacillus subtilisATCC 21216, andMicrococcus luteusATCC 4698), and six Gram-negative bacterial strains (Escherichia coliDH52,Escherichia coliJM109,Salmonella dysenteriae,Pseudomonas aeruginosaATCC 27853,Bacillus proteusATCC13315 andBacillus typhi) was carried out. These findings manifested that compound7cdisplayed excellent antifungal efficacy while compound7brevealed significant anti-microbial activity. In addition binding behaviour of compound7bwas investigated by binding study between calf thymus DNA and compound7bby UV–Vis absorption spectroscopy and further research about HSA interactions was carried out.Graphical AbstractDisplay OmittedHighlights?Green approach by means of water mediated multi-component synthesis?In-vitro anti-inflammatory activity via two different methods?In-vitro antimicrobial study through two fold serial dilution technique?Interaction behaviour of compound with calf thymus DNA?An interaction of HSA with compounds has been studied.]]>