Abstract

Bacterial infections, especially those caused by strains resistant to commonly used antibiotics and chemotherapeutics, are still a current threat to public health. Therefore, the search for new molecules with potential antimicrobial activity is an important research goal. In this article, we present the synthesis and evaluation of the in vitro antimicrobial activity of a series of 15 new derivatives of 4-methyl-1,2,3-thiadiazole-5-carboxylic acid. The potential antimicrobial effect of the new compounds was observed mainly against Gram-positive bacteria. Compound 15, with the 5-nitro-2-furoyl moiety, showed the highest bioactivity: minimum inhibitory concentration (MIC) = 1.95–15.62 µg/mL and minimum bactericidal concentration (MBC)/MIC = 1–4 µg/mL.

Highlights

  • Antibiotics have been one of the most dynamically developing groups of medicines of the last decade [1]

  • The first use of an antibiotic in the early 20th century became a landmark in treating infections

  • Hydrazones was confirmed by elemental analysis and the FT-IR, 1 H NMR, and 13 C NMR

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Summary

Introduction

Antibiotics have been one of the most dynamically developing groups of medicines of the last decade [1]. As a result of the common use of penicillin, a strain of Staphylococcus aureus bacterium appeared, which produced the penicillinase enzyme, giving it resistance to penicillin [3] In response to this fact, newer antibiotics were introduced as treatments. This group includes extremely virulent strains of methicillin-resistant S. aureus (MRSA) [3,8,9] This etiological agent is thought to be one of the most common causes of life-threatening infections in palliative care facilities and during inpatient treatment [10]. This problem has been noticed by key institutions and global and European public health organizations [1].

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