Thiosemicarbazones active against Clostridium difficile

Costello, Cait M.; Kärpänen, Tarja J.; Lambert, Peter A.; Mistry, Preena; Parker, Katy J.; Rathbone, Daniel L.; Ren, Jiangmeng; Wheeldon, L.J.; Worthington, Tony

doi:10.1016/j.bmcl.2008.01.041

Cited by 21 publications

(18 citation statements)

References 11 publications

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“…4 ) with promising activity in 2008 [240]. This compound was tested against a panel of clinically important organisms and showed a MIC of 4-8 µg/mL against the reference strain NCTC 11204 of C. difficile and MICs of 0.125-32 μg/mL against over 30 clinical strains tested.…”

Section: Newer Agents For CDImentioning

confidence: 99%

“…Moreover, it was largely inactive against the Gram-negative microorganism Acinetobacter spp. or C. albicans yeast strains [240]. …”

Section: Newer Agents For CDImentioning

confidence: 99%

“…The thiosemicarbazones were synthesized in two steps with yields of 59-93% for the nitrofuranyl compounds and 27-57% for the furanyl compounds [240]. Three other thiosemicarbazone compounds with noticeable antimicrobial activity all share the 5-nitrofuran heterocyclic moiety.…”

Section: Newer Agents For CDImentioning

confidence: 99%

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Progress in the Discovery of Treatments for C. difficile Infection: A Clinical and Medicinal Chemistry Review

Tsutsumi¹,

Owusu²,

Hurdle³

et al. 2013

CTMC

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Clostridium difficile is an anaerobic, Gram-positive pathogen that causes C. difficile infection, which results in significant morbidity and mortality. The incidence of C. difficile infection in developed countries has become increasingly high due to the emergence of newer epidemic strains, a growing elderly population, extensive use of broad spectrum antibiotics, and limited therapies for this diarrheal disease. Because treatment options currently available for C. difficile infection have some drawbacks, including cost, promotion of resistance, and selectivity problems, new agents are urgently needed to address these challenges. This review article focuses on two parts: the first part summarizes current clinical treatment strategies and agents under clinical development for C. difficile infection; the second part reviews newly reported anti-difficile agents that have been evaluated or reevaluated in the last five years and are in the early stages of drug discovery and development. Antibiotics are divided into natural product inspired and synthetic small molecule compounds that may have the potential to be more efficacious than currently approved treatments. This includes potency, selectivity, reduced cytotoxicity, and novel modes of action to prevent resistance.

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Section: Newer Agents For CDImentioning

confidence: 99%

“…Moreover, it was largely inactive against the Gram-negative microorganism Acinetobacter spp. or C. albicans yeast strains [240]. …”

Section: Newer Agents For CDImentioning

confidence: 99%

See 1 more Smart Citation

Progress in the Discovery of Treatments for C. difficile Infection: A Clinical and Medicinal Chemistry Review

Tsutsumi¹,

Owusu²,

Hurdle³

et al. 2013

CTMC

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“…For instance, thiosemicarbazones and their metal complexes represent an interesting class of compounds with a wide range of pharmacological applications [68]. Many examples of this class of compounds have been evaluated as having antitumor [69,70], antiviral [71], antiprotozoal [72,73], antibacterial [74,75] and antifungal [74,76] activities. In many cases upon coordination to metal ions, the bioactivity of these compounds increases, suggesting that complexation can be an interesting strategy of dose reduction [77][78][79][80][81].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, structures and antibacterial activities of benzoylthiourea derivatives and their complexes with cobalt

Yang

Liu

et al. 2012

Journal of Inorganic Biochemistry

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“…Incorporation of metals onto these thiosemicarbazone ligands can result in alteration or enhancement of their biological activity (Sampath and Jayabalakrishnan, 2013). The toxicological importance of the -N-C = S moiety has been well established in antifungal, antibacterial (Costello et al, 2008), and pesticidal activities. Cleavage of plasmid DNA has an efficiency order Me 3 Sn(…”

Section: Dna Cleavage Activitymentioning

confidence: 99%

Synthesis, characterization, antimicrobial, and DNA cleavage evaluation of some organotin(IV) complexes derived from ligands containing the 1H-indole-2,3-dione moiety

Sharma

Meena

Singh

et al. 2016

Main Group Metal Chemistry

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Sn), and ultraviolet-visible light spectroscopic studies. The spectroscopic data showed that the ligands are monobasic bidentate, coordinating through nitrogen and sulfur/oxygen atoms. Thus, suitable trigonal bipyramidal geometry and octahedral geometry have been suggested for the 1:1, and 1:2 metal complexes, respectively. The ligands and their complexes have been tested against various microbes for their in vitro antimicrobial activities. All complexes exhibit good antibacterial activity against the two bacterial species Escherichia coli and Staphylococcus aureus and remarkable antifungal activity against the two fungi Fusarium semitectum and Aspergillus flavus with respect to their corresponding ligands. The DNA cleavage efficiency of the ligands and the complexes has also been examined and discussed using gel electrophoresis technique, which showed the cleavage of DNA by all the metal complexes and ligands.

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Thiosemicarbazones active against Clostridium difficile

Abstract: A set of closely related furylidene thiosemicarbazones was prepared and screened against various clinically important Gram-positive bacteria. One compound containing an ethylene spacer and a 5-nitrofuryl group was found to have promising activity against Clostridium difficile.

Cited by 21 publications

References 11 publications

Progress in the Discovery of Treatments for C. difficile Infection: A Clinical and Medicinal Chemistry Review

Progress in the Discovery of Treatments for C. difficile Infection: A Clinical and Medicinal Chemistry Review

Synthesis, structures and antibacterial activities of benzoylthiourea derivatives and their complexes with cobalt

Synthesis, characterization, antimicrobial, and DNA cleavage evaluation of some organotin(IV) complexes derived from ligands containing the 1H-indole-2,3-dione moiety

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