Compounds containing 2-substituted imidazole ring for treatment against human African trypanosomiasis

Samant, Bhupesh S.; Sukhthankar, Mugdha

doi:10.1016/j.bmcl.2010.12.040

Cited by 22 publications

(16 citation statements)

References 15 publications

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“…The replacement of nitro group on the imidazole ring with other electron‐withdrawing groups such as Cl, Br, and SO 3 H failed to give any improved anti‐ T. brucei activity even increased cytotoxicity. However, the exact mechanism of action of this compound was still unknown …”

Section: Imidazoles As Antiparasitic Agentsmentioning

confidence: 99%

Comprehensive Review in Current Developments of Imidazole-Based Medicinal Chemistry

et al. 2013

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Imidazole ring is an important five-membered aromatic heterocycle widely present in natural products and synthetic molecules. The unique structural feature of imidazole ring with desirable electron-rich characteristic is beneficial for imidazole derivatives to readily bind with a variety of enzymes and receptors in biological systems through diverse weak interactions, thereby exhibiting broad bioactivities. The related research and developments of imidazole-based medicinal chemistry have become a rapidly developing and increasingly active topic. Particularly, numerous imidazole-based compounds as clinical drugs have been extensively used in the clinic to treat various types of diseases with high therapeutic potency, which have shown the enormous development value. This work systematically gives a comprehensive review in current developments of imidazole-based compounds in the whole range of medicinal chemistry as anticancer, antifungal, antibacterial, antitubercular, anti-inflammatory, antineuropathic, antihypertensive, antihistaminic, antiparasitic, antiobesity, antiviral, and other medicinal agents, together with their potential applications in diagnostics and pathology. It is hoped that this review will be helpful for new thoughts in the quest for rational designs of more active and less toxic imidazole-based medicinal drugs, as well as more effective diagnostic agents and pathologic probes.

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Section: Imidazoles As Antiparasitic Agentsmentioning

confidence: 99%

Comprehensive Review in Current Developments of Imidazole-Based Medicinal Chemistry

et al. 2013

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“…This was somewhat as recorded in the use of nitroimidazole, in the treatment of both acutely and chronically T. brucei infection in rats when administered per os at the dose of 25-50 mg kgG 1 for 4 days and at 50-100 mg kgG 1 for 5 days, respectively (Trunz et al, 2011). Similarly, in use of 2-substituted 5-nitroimidazoles such as fexinidazole and 1-[4-(1-methyl-5-nitro-1H-imidazol-2-ylmethoxy)-pyridin-2-yl-piperazine (9e) in treatment of invitro T. brucei in Human African Trypanosomosis (Samant and Sukhthankar, 2011). However, doses used in treatment of Babesia and Anaplasma species maybe tried on trypanosome infections in animals (Hashemi-Fesharki, 1975, 1977Kuttler, 1980).…”

Section: Discussionmentioning

confidence: 99%

Comparative Therapeutic Efficacy of Imidocarb Di-Propionate and Diminazene Aceturate in Rats Experimentally Infected with Trypanosoma brucei

Nwoha¹,

Omamegbe²

2015

Research J. of Veterinary Sciences

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Diminazene aceturate is a yellow to orange aromatic diamidine compound with both antibacterial and protozoal activities. Diminazene aceturate is one of the most important drugs used in the treatment of trypanosomosis in animals. It is often used in treatment of Babesia and Trypanosoma species in animals. Over the years, consistent use of diminazene aceturate especially at low doses by quacks made provisions for development of resistant strains of trypanosome species and relapses of infection few days post treatment. The present challenge in chemotherapy in trypanosomosis necessitated the search for alternative therapies in both humans and animal patients. This study experimentally demonstrates the efficacy of imidocarb dipropionate in treatment of trypanosomosis. Its administration at the dose of 24 mg kgG 1 subcutaneously for 2 consecutive days had a curative effect on rats with experimental Trypanosoma brucei infection. There was no relapse recorded in the treated group till the last (12th) day of the experiment. The present study threw some light on the potentials of imidazole dipropionate as an alternative therapy in trypanosomosis. It however requires a much detailed research to confirm its potency as a trypanocid.

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“…Among the several halonitrobenzamides derivatives synthesized by Hwang et al [220], and evaluated against a T. b. brucei culture compounds, compound 117 was found to be the most potent inhibitor (IC 50 = 1.5 µM). An assessment of the antiprotozoal activities (antitrypanosomal) of a series of nitroimidazole analogs developed by Samant et al [221] revealed that among the synthesized molecules, compound 118 was the most active antitrypanosomal agent (IC 50 = 0.25 µM). Ferrins et al [222] synthesized various anilides and the evaluation of their antitrypanosomal activity revealed that among the compounds synthesized, compound 119 (IC 50 = 0.091 µM) significantly inhibited a T. b. rhodesiense culture.…”

Section: Recent Progress Of Antiprotozoan Agentsmentioning

confidence: 99%

Recent Advances in the Discovery of Novel Antiprotozoal Agents

et al. 2019

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Parasitic diseases have serious health, social, and economic impacts, especially in the tropical regions of the world. Diseases caused by protozoan parasites are responsible for considerable mortality and morbidity, affecting more than 500 million people worldwide. Globally, the burden of protozoan diseases is increasing and is been exacerbated because of a lack of effective medication due to the drug resistance and toxicity of current antiprotozoal agents. These limitations have prompted many researchers to search for new drugs against protozoan parasites. In this review, we have compiled the latest information (2012–2017) on the structures and pharmacological activities of newly developed organic compounds against five major protozoan diseases, giardiasis, leishmaniasis, malaria, trichomoniasis, and trypanosomiasis, with the aim of showing recent advances in the discovery of new antiprotozoal drugs.

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Compounds containing 2-substituted imidazole ring for treatment against human African trypanosomiasis

Cited by 22 publications

References 15 publications

Comprehensive Review in Current Developments of Imidazole-Based Medicinal Chemistry

Comprehensive Review in Current Developments of Imidazole-Based Medicinal Chemistry

Comparative Therapeutic Efficacy of Imidocarb Di-Propionate and Diminazene Aceturate in Rats Experimentally Infected with Trypanosoma brucei

Recent Advances in the Discovery of Novel Antiprotozoal Agents

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