Abstract

The antimicrobial activity of 2-naphtholic and phenolic azo compounds was determined against seven microbial species, Staphylococcus aureus (ATCC 25923), Streptococcus pyrogenes (clinical), and Enterococcus faecalis (ATCC 29212), Salmonella typhi (clinical), Pseudomonas aeruginosa (ATCC 27853), Escherichia coli (ATCC 251922), and Candida albicans (ATCC 10231), using the high-throughput spot culture growth inhibition assay (HT-SPOTi). The minimum inhibitory concentrations (MIC) were determined for the active azo dyes. All the azo compounds (A1–B4) were screened for anthelmintic activity against adult Ghanaian earthworms, Hyperiodrilus spp. As part of the systematic investigation for biological activity, all the azo compounds exhibited good antimicrobial activity against the seven human pathogenic microorganisms. All the compounds exhibited anthelminthic activity against adult Ghanaian earthworms, Hyperiodrilus spp.

Highlights

  • Over the past decades, the emergence of resistant pathogens in humans has been on the ascendency and has become a global health concern in chemotherapy of infectious diseases [1]. is has stimulated efforts in the field of antimicrobial chemotherapy search for novel drugs to curtail this menace [2]

  • A section of neglected tropical diseases are associated with helminths, and they are amongst the most common ones affecting the world and posing major public health threat, contributing to high morbidity and mortality [3, 4]. e existence of few antimicrobials and anthelminthics coupled with current chemotherapy losing their efficacy calls for continuous research for new but more effective compounds in the drug discovery industry [5, 6]

  • We present our findings on the synthesis and in vitro antimicrobial and anthelminthic evaluation of naphtholic and phenolic azo dyes derived from the coupling of various primary aromatic amines with 2-naphthol and phenol

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Summary

Introduction

The emergence of resistant pathogens in humans has been on the ascendency and has become a global health concern in chemotherapy of infectious diseases [1]. is has stimulated efforts in the field of antimicrobial chemotherapy search for novel drugs to curtail this menace [2]. E existence of few antimicrobials and anthelminthics coupled with current chemotherapy losing their efficacy calls for continuous research for new but more effective compounds in the drug discovery industry [5, 6]. Typical examples of azo dye compounds which are drugs include phenazopyridine, which is a urinary tract analgesic, and sulfasalazine for inflammatory bowel disease (Figure 1). They are synthetically feasible by simple standard diazotisation and coupling reactions, there is still more to be carried out with regards to Journal of Tropical Medicine. Scheme 1 represents a general synthetic pathway for the azo dyes with their proposed names. e eight azo compounds are [A1] (E)-4-((2-hydroxynaphthalen-1-yl) diazenyl) benzoic acid, [A2] (E)-1-((4-chlorophenyl) diazenyl) naphthalen-2-ol, [A3] (E)-ethyl 4-((2-hydroxynaphthalen-1-yl) diazenyl) benzoate, [A4] (E)-4-((2hydroxynaphthalen-1-yl) diazenyl) benzene sulphonamide, [B1] (E)-4-((4-hydroxyphenyl) diazenyl) benzoic acid, [B2] (E)-ethyl 4-((4-hydroxyphenyl) diazenyl) benzoate, [B3] (E)-4-((2-chloro-4-nitrophenyl) diazenyl) phenol, and [B4] (E)-4-(4-nitrophenyl) diazenyl) phenol. ese compounds are coded based on their reacting components and are shown in Table 1. e synthesised azo compounds were investigated for their antimicrobial and anthelminthic activities

Materials and Methods
Step II
Antimicrobial Activity
Step I
Step III
Anthelminthic Activity
A2 A3 A4 B1 B2 B3 B4 Ciprofloxacin Cefuroxime Amoxicillin Fluconazole
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