Abstract

Introduction: In recent times, most of the currently available antimicrobial agents have developed resistance. Extensive pharmacological activities including bactericidal and bacteriostatic nature of flavonoids, made them as priority agents in this aspect of research study. Synthetic flavonoids such as hydroxy thiophen derivatives were considered to evaluate for antimicrobial activity in this study. 
 Objective: The present study involves the analysis for antimicrobial activity of thiophen substituted synthetic flavonoids.
 Methods: Claisen-Schmidt method of condensation fallowed by oxidative cyclization reactions from substituted hydroxyacetophenone with aromatic aldehydes were used to synthesize the various analogues of flavonoid compounds. Then these compounds after their FTIR, 1H NMR, MS spectral characterization and elemental analysis, were screened for in vitro antibacterial and antifungal activity by using disc diffusion method followed by determining their respective zone of inhibitions.
 Results: All the synthesized test flavonoid compounds exhibited the good antibacterial and antifungal spectrum activity over B. subtilis, S. aureus, E. coli and P. aeurugenosa bacteria and Candida albicans and Aspergillus niger fungal microbes. However compounds such as F1, F2 and F4 showed moderately significant antibacterial activity against P. aerugenosa organism than the other test compounds and the same F1 and F2 test compounds exhibited significant antifungal activity at100µg concentration.
 Conclusion: The present study demonstrated that the novel thiophen substituted flavonoids (F1, F2, F3 and F4 ) found to have promising antimicrobial and antifungal activity which needs to be confirmed by in vivo studies.

Highlights

  • In recent times, most of the currently available antimicrobial agents have developed resistance.Extensive pharmacological activities including bactericidal and bacteriostatic nature of flavonoids, made them as priority agents in this aspect of research study

  • Claisen-Schmidt method of condensation fallowed by oxidative cyclization reactions from substituted hydroxyacetophenone with aromatic aldehydes were used to synthesize the various analogues of flavonoid compounds

  • 2.1 Chemistry: Condensation fallowed by oxidative cyclization reaction was used to synthesize the flavonoids according to method of Algar-Flynn-Oyamada reaction [17,18,19]. 2-Hydroxy acetophenone in methanol under aqueous alkali media, was refluxed with different substituted benzaldehyde, to obtain 70–80% of corresponding chalcones yield

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Summary

Introduction

Most of the currently available antimicrobial agents have developed resistance. Extensive pharmacological activities including bactericidal and bacteriostatic nature of flavonoids, made them as priority agents in this aspect of research study. Synthetic flavonoids such as hydroxy thiophen derivatives were considered to evaluate for antimicrobial activity in this study. Developing countries declared that there is alarming increase of antibiotic resistance among pathogenic bacteria. There is need for discovery of new antimicrobial drugs or leads as the number of microbes developing resistance to existing antimicrobial drugs is increasing and spreading worldwide [2]. R.S. Keri et al 2017 reported that, replacement of phenyl ring by thiophen moiety resulted in the increase of biological activity. Keri et al 2017 reported that, replacement of phenyl ring by thiophen moiety resulted in the increase of biological activity. [6]

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