Abstract

Several nicotinic and isoniazid derivatives, most of them containing nitro groups were synthesized by our group, and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv using the Alamar Blue susceptibility test and the activity expressed as the minimum inhibitory concentration (MIC) in mg/mL. The compound 11d exhibited the best result (1.2 µg/mL) when compared with first line drugs such as isoniazid (INH) and rifampicin (RIP). Therefore this class of compounds could be a good starting point to develop new lead compounds in the treatment of multi-drug resistant tuberculosis.

Highlights

  • The pyridine nucleus is an important heteroaromatic class of compounds with a wide range of activities and it is present in many products such as drugs, vitamins, food, flavorings, plants, dyes, rubber products, adhesives, insecticides and herbicides[1]

  • Of anti-tuberculosis first-line drug isoniazid[5], which is an analogue of isonicotinic acid, an isomer of nicotinic acid

  • Due to the importance of nicotinic acid derivatives and its isomers, the aim of this article is to evaluate the in vitro antibacterial activity against Mycobacterium tuberculosis of several compounds of this class synthesized by our group

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Summary

Introduction

The pyridine nucleus is an important heteroaromatic class of compounds with a wide range of activities and it is present in many products such as drugs, vitamins, food, flavorings, plants, dyes, rubber products, adhesives, insecticides and herbicides[1] In this context, nicotinic acid (pyridine-3-carboxylic acid), known as niacin and vitamin B3, is found in various plants and animals and has vital roles in such biological processes as production of energy, signal transduction, regulation of gene expression and synthesis of fatty acids, cholesterol and steroids[2,3]. Nicotinic acid derivatives and its isomers have been investigated as an agent for the prevention or delay of the onset of type 1 diabetes mellitus[4] They have anti-bacterial, anti-oxidant, anti-inflammatory and anti-carcinogenic activities, and have putative activity against osteoarthritis and granuloma annulare[3]. Due to the importance of nicotinic acid derivatives and its isomers, the aim of this article is to evaluate the in vitro antibacterial activity against Mycobacterium tuberculosis of several compounds of this class synthesized by our group

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