New Hydrazones Bearing Thiazole Scaffold: Synthesis, Characterization, Antimicrobial, and Antioxidant Investigation.

Cristina Nastasă,Ovidiu Oniga,Brîndușa Tiperciuc,Daniela Benedec,Mihaela Duma

doi:10.3390/molecules200917325

Abstract

New series of hydrazones 5–18 were synthesized, in good yields, by reacting 4-methyl-2-(4-(trifluoromethyl)phenyl)thiazole-5-carbohydrazide with differently substituted benzaldehyde. The resulting compounds were characterized via elemental analysis, physico-chemical and spectral data. An antimicrobial screening was done, using Gram (+), Gram (−) bacteria and one fungal strain. Tested molecules displayed moderate-to-good growth inhibition activity. 2,2-Diphenyl-1-picrylhydrazide assay was used to test the antioxidant properties of the compounds. Monohydroxy (14–16), para-fluorine (13) and 2,4-dichlorine (17) derivatives exhibited better free-radical scavenging ability than the other investigated molecules.

Highlights

IntroductionFor more than a few decades, a threat to the effectiveness of common therapy
Microbial resistance has been, for more than a few decades, a threat to the effectiveness of common therapy
The combination of thiazole- and hydrazone-type compounds might provide new effective drugs for the treatment of multidrug resistant microbial infections and for diminishing oxidative processes. Prompted by all these relevant data, we propose here the synthesis of new hybrid molecules, which gather the two pharmacophores, and the investigation of their antimicrobial and antioxidant potential

Summary

Introduction

For more than a few decades, a threat to the effectiveness of common therapy. In the case of patients at risk, this can involve the extension of the disease or even death [1,2,3,4]. Pathogens have developed several types of resistance (natural/intrinsic and acquired) and different installation mechanisms. The most alarming resistance to conventional treatment is cited for nine bacteria: Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus, Streptococcus pneumoniae, Salmonella and Shigella species, Neisseria gonorrhoeae. Candida species infections are a public health problem worldwide, the most common form of fungal infection. Invasive forms have high rate of morbidity and mortality, especially in patients with cancer, immunocompromise, new-borns, or those in the intensive care unit. There is reported increased resistance to azoles (fluconazole) and the emergence of strains resistant to echinocandins, the newest class of antifungal agents [5]

Methods

Results

Conclusion