Abstract
Increased bacterial resistance to antibiotics is a major threat to human health, and it is particularly important to develop novel antibiotic drugs. Here, we designed a series of Schiff base thiosemicarbazone derivatives containing an adamantane moiety, and carried out the structural characterization of the compounds and in vitro antibacterial activity tests. Compound 7e was as effective as the commonly used antibiotic ampicillin against the Gram-negative bacterium Escherichia coli, and compound 7g had a good inhibitory effect against Gram-positive Bacillus subtilis. These findings provide data for the development of better thiosemicarbazone antibacterial agents.
Highlights
In the past 30 years, only limited progress has been made in research into antibacterial drugs with new mechanisms and core structures [1,2,3]
Scheme 1 shows the procedure for synthesis of novel Schiff base derivatives of thiosemicarbazones with an adamantane moiety
The structures of thiosemicarbazone compounds 7a-h were confirmed on the basis of infrared (IR), 1H nuclear magnetic resonance (NMR), 13C NMR, and electrospray ionization mass spectral (ESI/MS) data, which showed their negative ion peaks [M + H]+
Summary
In the past 30 years, only limited progress has been made in research into antibacterial drugs with new mechanisms and core structures [1,2,3]. Toxicity and bacterial resistance to the drugs play an important role in the failure of treatment [4, 5]. The development of antibacterial drugs with novel structures is very important research for clinical application [6]. Compounds with a thiosemicarbazone structure are known to possess tranquilizing, muscle relaxing, psychoanaleptic, hypnotic, ulcerogenic, antidepressant, antibacterial, antifungal, analgesic, and anti-inflammatory properties [7,8,9,10,11,12,13,14]. Thiosemicarbazones are a type of Schiff base formed by condensation of thiosemicarbazide and an aldehyde or ketone. Studies have shown that changing the structure of the aldehydes and ketones or introducing different active groups on position N(4) can improve the antibacterial and anticancer activities of the compounds [15]
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