Novel Derivatives of 4-Methyl-1,2,3-Thiadiazole-5-Carboxylic Acid Hydrazide: Synthesis, Lipophilicity, and In Vitro Antimicrobial Activity Screening

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 mu g/mL and minimum bactericidal concentration (MBC)/MIC = 1-4 mu g/mL.

Automated summary

Bacterial infections, especially those caused by resistant strains, pose a threat to public health. The search for new molecules with antimicrobial activity is important. A series of 15 new derivatives showed potential antimicrobial effects against Gram-positive bacteria, with compound 15 exhibiting the highest bioactivity.