Antiparasitic Drugs. Iv. 2-(4'-Thiazolyl)-Benzimidazole, a New Anthelmintic

Brown, Heloise; Matzuk, A. R.; Ilves, I. R.; Peterson, Louis H.; Harris, Simon; Sarett, L. H.; Egerton, J. R.; Yakstis, J. J.; Campbell, William C.; Cuckler, A. C.

doi:10.1021/ja01468a052

Cited by 224 publications

(76 citation statements)

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“…S1) were used as broad-spectrum anthelmintics in various animal species. TBZ, a kind of benzimidazole with broad anthelmintic activity, is effective in the treatment of various nematode infections in humans and animals (Brown et al, 1961;Cuckler, 1961;Ames et al, 1963;Portugal et al, 2002;Igual-Adell et al, 2004) and shows highly effective against a variety of fungi (Robinson et al, 1978). Pentachlorophenol is an organochlorine compound that was first produced in the 1930s and used as a herbicide, insecticide, fungicide, algaecide, disinfectant and as an ingredient in antifouling paint, was found to be a potent inhibitor of E. coli SQR and QFR (Maklashina and Cecchini, 1999;Ruprecht et al, 2009) and bovine SQR (Afanas'eva and Kostyrko, 1986).…”

Section: Introductionmentioning

confidence: 99%

Thiabendazole inhibits ubiquinone reduction activity of mitochondrial respiratory complex II via a water molecule mediated binding feature

et al. 2011

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The mitochondrial respiratory complex II or succinate: ubiquinone oxidoreductase (SQR) is a key membrane complex in both the tricarboxylic acid cycle and aerobic respiration. Five disinfectant compounds were investigated with their potent inhibition effects on the ubiquinone reduction activity of the porcine mitochondrial SQR by enzymatic assay and crystallography. Crystal structure of the SQR bound with thiabendazole (TBZ) reveals a different inhibitor-binding feature at the ubiquinone binding site where a water molecule plays an important role. The obvious inhibitory effect of TBZ based on the biochemical data (IC 50~1 00 μmol/L) and the significant structure-based binding affinity calculation (~94 μmol/L) draw the suspicion of using TBZ as a good disinfectant compound for nematode infections treatment and fruit storage.

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Section: Introductionmentioning

confidence: 99%

Thiabendazole inhibits ubiquinone reduction activity of mitochondrial respiratory complex II via a water molecule mediated binding feature

et al. 2011

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“…Thiabendazole was the first of the benzimidazoles, which were to become the blockbuster broad-spectrum anthelmintics of their day (24). Its anthelmintic efficacy was discovered empirically in assays conducted by my colleague Dr. John R. Egerton, using nematode larvae in vitro and nematode infections in mice.…”

Section: Lessons From the General History Of Antiparasitic Drugsmentioning

confidence: 99%

Lessons from the History of Ivermectin and Other Antiparasitic Agents

Campbell

2016

Annu. Rev. Anim. Biosci.

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The twentieth century's arsenal of chemical anthelmintics brought manifold improvement in human health and, more abundantly, in animal health. The benefits were not only in health per se but also in agricultural economics, livestock management, and the overall production of food and fiber to support expanding human populations. Nevertheless, there remains (due in large part to drug resistance and paucity of available vaccines) a great need for new means of controlling disease caused by parasitic worms. Prudence should persuade us to look to our past for lessons that might help in our quest for new drugs. The lessons suggested here derive from the history of ivermectin and other anthelmintics. They deal with the means of finding substances with useful antiparasitic activity and with alternative approaches to drug discovery.

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“…The successes have been cyclical and directly related to the timely introduction of new drugs as resistance to older drugs has surfaced. Effective drug utilization dates back to the 1960s with development of benzimidazoles (BZ) (Brown et al, 1961), followed by the imidothiazoles-tetrahydropyrimidines in the 1970s, and the production of macrocyclic lactones (avermectins and milbemycin) in the 1980s (Chabala et al, 1980). The first cyclodepsipeptide (Sasaki et al, 1992) was commercially introduced for nematode control in cats in 2006.…”

Section: Chemotherapymentioning

confidence: 99%

Parasitic nematodes—From genomes to control

Mitreva

Zarlenga

McCarter

et al. 2007

Veterinary Parasitology

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The diseases caused by parasitic nematodes in domestic and companion animals are major factors that decrease production and quality of the agricultural products. Methods available for the control of the parasitic nematode infections are mainly based on chemical treatment, non-chemical management practices, immune modulation and biological control. However, even with integrated pest management that frequently combines these approaches, the effective and long-lasting control strategies are hampered by the persistent exposure of host animals to environmental stages of parasites, the incomplete protective response of the host and acquisition of anthelmintic resistance by an increasing number of parasitic nematodes. Therefore, the challenges to improve control of parasitic nematode infections are multi-fold and no single category of information will meet them all. However, new information, such as nematode genomics, functional genomics and proteomics, can strengthen basic and applied biological research aimed to develop improvements.In this review we will, summarize existing control strategies of nematode infections and discuss ongoing developments in nematode genomics. Genomics approaches offer a growing and fundamental base of information, which when coupled with downstream functional genomics and proteomics can accelerate progress towards developing more efficient and sustainable control programs. #

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Antiparasitic Drugs. Iv. 2-(4'-Thiazolyl)-Benzimidazole, a New Anthelmintic

Cited by 224 publications

References 0 publications

Thiabendazole inhibits ubiquinone reduction activity of mitochondrial respiratory complex II via a water molecule mediated binding feature

Thiabendazole inhibits ubiquinone reduction activity of mitochondrial respiratory complex II via a water molecule mediated binding feature

Lessons from the History of Ivermectin and Other Antiparasitic Agents

Parasitic nematodes—From genomes to control

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