Abstract

Novel substituted 1,2,4-dithiazolylchromones 3a–j were synthesized by the reaction of 3-formylchromones (1a–j) with two equivalents of p-chlorothiobenzamide (2) in dry xylene and characterized spectroscopically (IR, 1H and 13C NMR, mass) and elemental analysis. All synthesized compounds were screened for in vitro antimicrobial activity against various pathogenic bacterial and fungal strains and were found to possess good to moderate inhibitory potential against all tested strains. Antimicrobial results reveal that compounds bearing lipophilic electron withdrawing groups such as chloro and bromo displayed significant inhibitory potential against both bacterial and fungal strains. Particularly, compound 3c displayed significant inhibitory against bacterial strains and compound 3h exhibits significant inhibitory potential in comparison to standard drug fluconazole against fungal strain S. cerevisiae.

Highlights

  • Fungal and bacterial infections are affecting millions of people worldwide, and are associated with high rates of mortality and morbidity [1]

  • We have reported the synthesis of 3-(5-phenyl3H-[1,2,4]-dithiazol-3-yl) chromen-4-ones with significant inhibitory potential against microbial strains; compound having both electron withdrawing groups such as chloro and fluoro linked with chromone ring showed more inhibitory potential against fungal strains than standard drug [12]

  • It was decided in the present study to incorporate chloro group at the phenyl ring of the 1,2,4dithiazolylchromones in order to observe the effect of novel substitution on antimicrobial activity

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Summary

Introduction

Fungal and bacterial infections are affecting millions of people worldwide, and are associated with high rates of mortality and morbidity [1]. We have reported the synthesis of 3-(5-phenyl3H-[1,2,4]-dithiazol-3-yl) chromen-4-ones with significant inhibitory potential against microbial strains; compound having both electron withdrawing groups such as chloro and fluoro linked with chromone ring showed more inhibitory potential against fungal strains than standard drug [12]. It was decided in the present study to incorporate chloro group at the phenyl ring of the 1,2,4dithiazolylchromones in order to observe the effect of novel substitution on antimicrobial activity

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