Design synthesis and in vitro evaluation of novel potent biologically active benzothiazole based bio conjugates

Abstract

newline xvi newlineABSTRACT newlineMicro-organism resistance to drugs is well known and has made it necessary to explore newlinenovel therapeutic agents that have a multi-target mode of action, low resistance, high newlinetolerance and no adverse effect. Towards that effort we have synthesized the bioconjugates newlineof benzothiazole derivatives with N-acetyl-D-glucosamine (NAG), biscoumarin, newlinedihydropyrimidine and cystine through an ester linkage. All the synthesized newlinecompounds were prepared via environment-friendly and through green processes, and in newlinegood concord with elemental and spectral data such as FTIR, 1H NMR, 13C NMR, MASS newlineand elemental analysis. All compounds displayed potent effect against pathogenic microorganism newline(E. coli, S. aureus and C. albicans). The newly synthesized compounds and bioconjugates newlineof benzothiazole were also evaluated for anticancer (Hep-2 and caco cell lines) newlineactivity and antioxidant activity. Bio-conjugates were appraised more effective to newlinesuppress pathogenic microorganism infections in-vitro relative to equivalent doses of newlinenon-conjugated benzothiazole. newlineIn the present study, results outcome support that integration of bio-components (Nacetyl- newlineD-glucosamine, bis-coumarin, dihydropyrimidine and cystine) with newlinebenzothiazole giving a synergistic effect. Results confirmed a reduction in MICs value newlinefrom 25 to 1.25 and#956;g mL-1 against all the tested strains. MICs values were also newlinesignificantly lower in range in a comparison to standards antibiotics. Exploration of these newlineresults further confirmed that N-acetyl-D-glucosamine, bis-coumarin and newlinedihydropyrimidine based series are more potent in contrast to cystine conjugates. newlineFurthermore, CFU (cell forming unit) study results also proved 99.9% bacterial reduction newlineand bactericidal effect after 48 h in bio-conjugates against tested strains. In addition, newlineN-acetyl-D-glucosamine, bis-coumarin and dihydropyrimidine based bio-conjugates newlinewere also proved potent for antioxidant activity by cyclic voltammetry method. In newlinespecific, Cl-glu-03, N-BIS-03 and Me-DHP-03 conjugates signified ma