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Thiabendazole
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Thiabendazole is a 2-substituted benzimidazole with fungicidal and anthelminthic (parasiticidal) properties. It is also a chelating agent, which means that this agent is used medicinally to bind metals in cases of metal poisoning, such as lead, mercury or antimony. Thiabendazole is indicated for the treatment of strongyloidiasis (threadworm), cutaneous larva migrans (creeping eruption), visceral larva migrans, and trichinosis.
Hits and Lead Discovery in the Identification of New Drugs against the Trypanosomatidic Infections
Published in Venkatesan Jayaprakash, Daniele Castagnolo, Yusuf Özkay, Medicinal Chemistry of Neglected and Tropical Diseases, 2019
Theodora Calogeropoulou, George E. Magoulas, Ina Pöhner, Joanna Panecka-Hofman, Pasquale Linciano, Stefania Ferrari, Nuno Santarem, Ma Dolores Jiménez-Antón, Ana Isabel Olías-Molero, José María Alunda, Anabela Cordeiro da Silva, Rebecca C. Wade, Maria Paola Costi
Bhambra et al. (2016) reported the synthesis of a small library of 2,6-disubstituted-4,5,7- trifluorobenzothiophenes. Compounds 103 and 104 (Figure 37) demonstrated attractive antitrypanosomal activity against T. b. rhodesiense with IC50 values 0.60 and 0.53 μM, respectively, and no toxicity to mammalian cells. It is apparent that the activity of these compounds can be attributed to the existence of the benzimidazole moiety since its replacement resulted in loss of activity. Structures of potential hits 103 and 104.
Hymenolepis
Published in Dongyou Liu, Handbook of Foodborne Diseases, 2018
Current drugs for treating Hymenolepis infection include praziquantel, niclosamide, nitazoxanide, and benzimidazoles (e.g., albendazole and mebendazole). Praziquantel impairs tegument and causes vacuolization in the neck region of Hymenolepis. Niclosamide inhibits parasite glucose uptake. Nitazoxanide interferes with the pyruvate-ferredoxin oxidoreductase enzyme-dependent electron transfer reaction involved in anaerobic energy metabolism. Benzimidazoles interact with parasite tubulin, leading to inhibition of microtubule polymerization as well as glucose uptake.
Novel therapeutic opportunities for Toxoplasma gondii, Trichomonas vaginalis, and Giardia intestinalis infections
Published in Expert Opinion on Therapeutic Patents, 2023
Francesca Arrighi, Arianna Granese, Paola Chimenti, Paolo Guglielmi
Giardia intestinalis infection shares with T. vaginalis the employment of the 5-nitroimidazole class for its management, albeit no standardized treatment is still recommended for giardiasis [25]. Another class of drugs employed in giardiasis treatment is benzimidazoles, with albendazole and mebendazole being the most used ones (Figure 2) [58]. Even in this case, the employment of these drugs is not devoid of side effects; over the above reported ones for 5-nitroimidazoles, benzimidazoles, often employed in a single dose for 7 days, provoke side effects such as nausea, vomiting, diarrhea, and abdominal pain, and its use requires attention during pregnancy because it could have teratogenic outcomes. Along with side effects, multiple resistance mechanisms have developed. In the light of the above, the search for novel effective drugs able to eradicate trichomoniasis as well as giardiasis is still an urgent need.
Molecular design, synthesis and biological evaluation of novel 1,2,5-trisubstituted benzimidazole derivatives as cytotoxic agents endowed with ABCB1 inhibitory action to overcome multidrug resistance in cancer cells
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Abeer H. A. Abdelhafiz, Rabah A. T. Serya, Deena S. Lasheen, Nessa Wang, Mansour Sobeh, Michael Wink, Khaled A. M. Abouzid
Benzimidazole is a privileged scaffold which is incorporated in various bioactive compounds that reveal a wide range of biological activities and commonly used as anticancer, antihypertensive, antiviral, antifungal and anti-HIVs agents17. The benzimidazole scaffold is frequently used in many anticancer agents18,19 (Figure 2) such as bendamustine (4)20. Also, several benzmidazole based compounds exhibited an anticancer activity such as albendazole (5)21, carbendazim (6)22, tilomisole (Wy-18,251) (7)23. Moreover, some 2-substituted benzimidazole derivatives such as (8–10)24, (11)25 and (12)26 displayed a well tolerated anticancer activity in the cytotoxicity assays. Remarkably, the potent antiproliferative activity of the 2-(benzimidazol-2-yl)thio derivative (11) was apparent against colon cancer cells25. Interestingly, the 2,5-disubstituted benzimidazole derivative BD9L1 (12) displayed a substantial antiproliferative effects across a panel of cancer cell lines mainly CCRF/CEM leukaemia cells26.
Investigation of the toxicological and inhibitory effects of some benzimidazole agents on acetylcholinesterase and butyrylcholinesterase enzymes
Published in Archives of Physiology and Biochemistry, 2021
Antiparasitic drugs such as benzimidazoles are used in the prevention and treatment of parasitic diseases in animals, and the prominence of these drugs is increasing for animals that feed externally (Turkan et al.2019a). Some benzimidazoles derivatives such as ricobendazole, thiabendazole, albendazole and oxfendazole are some important antiparasitic drugs (Turkan et al. 2018a). These antiparasitic drugs are common drugs and used on animals. Various new benzimidazole derivatives have been developed which are used for the enhancing of antiparasitic activity and for the change of pharmacokinetic properties (Liang, Wang and Wang 2015, Nishida et al.1970, Gondolova et al.2018, Taslimi et al.2018c, Cetin et al.2019, Ekinci Akdemir et al.2016). The drugs in the benzimidazole class are widely used in the prevention and treatment of parasitic diseases in veterinary medicine (Türkan et al. 2018b).