Antibacterial Properties of 2-Acetylpyridine-1-Oxide Thiosemicarbazones

Abstract

We have investigated the in vitro antibacterial activity of 13 2-acetylpyridine-1-oxide thiosemicarbazones and 5 thiosemicarbazides against 80 clinically significant bacterial cultures, including 13 isolates with known antibiotic resistance. Of the thiosemicarbazones tested, 5 had minimal inhibitory concentrations (MICs) of 0.25 μg/ml for Neisseria gonorrhoeae isolates; 1 of these had an MIC range of 0.25–0.5 μg/ml for the Neisseria meningitidis cultures, and 2 had MICs of 2 and 2–4 μg/ml for Staphylococcus aureus and Streptococcus faecalis isolates, respectively. Two of the thiosemicarbazides had MICs of 0.25 μg/ml for N. gonorrhoeae, whereas 2 others had MICs of 2–4 and 4–8 μg/ml for S. aureus and S. faecalis isolates, respectively. The test compounds were ineffective against the gram-negative enteric cultures and the Pseudomonas isolates.

Nickel (II) complexes of naphthaquinone thiosemicarbazone and semicarbazone: Synthesis, structure, spectroscopy, and biological activity

“…Thiosemicarbazones (TSCs) have received considerable attention because of their potential therapeutic activities against bacterial and viral infections [1,2], tuberculosis [3] and leprosy [4]. In addition particular attention has been given to their antitumor activity that seems to be due to inhibition of DNA synthesis caused by a modification in the reductive conversion of ribonucleotides to deoxyribonucleotides [5].…”

Copper complexes of imidazole-2-, pyrrole-2- and indol-3-carbaldehyde thiosemicarbazones: Inhibitory activity against fungi and bacteria

“…Since then, this and other biological properties of thiosemicarbazones have been described [2]. It has been proposed [3][4][5][6] that antibacterial and fungicidal activity lie in their ability to chelate the essential metals, which the microorganisms need in their metabolism. Although their mechanism of action is still unclear, some copper complexes of thiosemicarbazones are of great interest because they show higher biological activity than their corresponding free thiosemicarbazones [7].…”

Cyanoacetic Acid Hydrazones of 3‐(and 4‐)Acetylpyridine and Some Derived Ring Systems as Potential Antitumor and Anti‐HCV Agents

“…Thiosemicarbazones (TSC), particularly those derived from 2-acetyl and 2-formyl pyridine, represent an interesting class of bioactive compounds due to their recorded antibacterial [1], antimalarial [2], antiviral [3,4], and antineoplastic [5,6] activities. These compounds have been shown to inhibit many enzyme activities in the nucleic acid metabolism [7][8][9].…”