Abstract

A series of potential bioactive compounds, N-(4-(aryl)-2-thioxo-1,3-thiazol-3(2H)-yl) pyridine-4-carboxamide has been synthesized and screened for antibacterial, antifungal, anti-inflammatory activity by minimum inhibitory concentration and protein denaturation method respectively. The compounds IIc and IIj were found to be broad spectrum antimicrobial agents at minimum inhibitory concentration value against E. coli, K. pneumonia, S. aureus, B. subtilis, A. nigar, and S. cerevisiae respectively. In anti-inflammatory activity, compounds IIc, IIf, IIh, and IIj at 100 mg/ml and compound IIl at 200 mg/ml were found significant active agent.

Highlights

  • There has been a constant battle between humans and the multitude of microorganisms that cause infections and diseases; the treatment of bacterial infections remains a challenging job because of the increasing number of multidrug-resistant microbial pathogens

  • Mentioned facts prompted us to synthesis a series of N-(4-(aryl)-2-thioxo-1,3-thiazol3(2H)-yl)pyridine-4-carboxamide compounds having antimicrobial and anti-inflammatory activity

  • FT-IR spectra were recorded in KBr on Bruker FT-IR instrument (Germany), 1H-NMR spectra were recorded on Bruker Avance 1H-NMR spectrometer (Germany), at 400 MHz in DMSO-d6, by using varian instrument using TMS as internal standard and chemical shift values are given in ppm downfield to TMS, GC Mass were recorded on GCMS-QP-5050 Schimadzu (Japan), and Perkin Elmer 2400 Series II CHN Elemental Analyzer

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Summary

Introduction

There has been a constant battle between humans and the multitude of microorganisms that cause infections and diseases; the treatment of bacterial infections remains a challenging job because of the increasing number of multidrug-resistant microbial pathogens. Despite the many chemotherapeutics available, the emergence of old and new antibiotic-resistant bacterial strains, mutations in microbial genomes, the incorrect use of antibiotics has been thoroughly demonstrated to greatly increase the development of resistant genotypes has generated a substantial need for new classes of anti-bacterial agents [1,2]. Various 2-thioxo-1,3-thiazol have been extensively investigated due to their application in different areas of biological activity such as antimicrobial [2,3], hypoglycemic [4], anti-inflammatory and analgesic agents [5], antidiabetic [6], antihyperglycemic [7]. Mentioned facts prompted us to synthesis a series of N-(4-(aryl)-2-thioxo-1,3-thiazol3(2H)-yl)pyridine-4-carboxamide compounds having antimicrobial and anti-inflammatory activity.

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