Abstract

Drug resistance causes serious difficulties in the routine therapy for curing common microbial infections. Thus it is very essential to develop new antimicrobial agents which can offer alternative treatments. The development of potent and effective antimicrobial agents is of utmost importance to overcome the emerging multidrug resistance strains of bacteria and fungi. The technique involves Knoevenagel reaction between substituted salicylaldehyde and ethyl acetoacetate in presence of piperidine as catalyst to give 3-acetyl coumarin. The intermediate coumarinyl chalcones was synthesized by condensing with various substituted benzaldehyde in presence of ethanolic KOH. The final synthesized pyridine-3-carbonitrile derivative was prepared upon refluxing with coumarinyl chalcones with malononitrile in presence of ammonium acetate. All the newly synthesized compounds were assigned on the basis of IR, 1H NMR and mass spectral data. The finalsynthesized compounds were screened for their antibacterial activity tube dilution method. Most of the compounds showed promising MIC by tube dilution method as compared to standard Cephalosporin.

Highlights

  • Drug-resistant infections kill more than 700,000 people each year and the number could increase to 10 million per year by 2050 in the world

  • The number of multi-drug resistant microbial strains and the appearance of strains with reduced susceptibility to antibiotics are continuously increasing. This increase has been attributed to indiscriminate use of broad-spectrum antibiotics, immunosuppressive agent, intravenous catheters, organ transplantation and ongoing epidemics of HIV infection. [1,2,3] According to Centers for Disease Control and Prevention (CDC) report, each year more than 2.8 million antibiotic infections occur and more than 35,000 people die as a result of these infections in the United States alone

  • The different Pyridine-3-Carbonitrile derivatives were evaluated for their antibacterial activity by Tube dilution method.The lowest concentration of the substance that prevents the development of visible growth was reported as the minimal inhibitory concentration (MIC) value.The newly prepared derivatives have different substituents, and they can exhibit antimicrobial activity

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Summary

Introduction

Drug-resistant infections kill more than 700,000 people each year and the number could increase to 10 million per year by 2050 in the world. The number of multi-drug resistant microbial strains and the appearance of strains with reduced susceptibility to antibiotics are continuously increasing. This increase has been attributed to indiscriminate use of broad-spectrum antibiotics, immunosuppressive agent, intravenous catheters, organ transplantation and ongoing epidemics of HIV infection. [1,2,3] According to Centers for Disease Control and Prevention (CDC) report, each year more than 2.8 million antibiotic infections occur and more than 35,000 people die as a result of these infections in the United States alone. The bacteria comprising biofilms are more resistant to antibiotics and the host immune system by a variety of mechanisms [5]

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