New series of imidazoles showed promising growth inhibitory and curative potential against trypanosoma infection

Oluyomi Stephen Adeyemi, Nthatisi Innocentia Molefe-Nyembe, Abiodun Omokehinde Eseola, Winfried Plass, Oluwatosin Kudirat Shittu, Ibrahim Olatunji Yunusa, Olubunmi Atolani, Ikponmwosa Owen Evbuomwan, Oluwakemi J. Awakan, Keisuke Suganuma, Kentaro Kato

    Research output: Contribution to journalArticlepeer-review

    Abstract

    The Trypanosoma spp. cause animal and human trypanosomiasis characterized with appreciable health and economic burden mostly in developing nations. There is currently no effective therapy for this parasitic disease, due to poor drug efficacy, drug resistance, and unwanted toxicity, etc. Therefore, new anti-Trypanosoma agents are urgently needed. This study explored new series of imidazoles for antiTrypanosoma properties in vitro and in vivo. The imidazoles showed moderate to strong and specific action against growth of T. congolense. For example, the efficacy of the imidazole compounds to restrict Trypanosoma growth in vitro was ≥ 12-fold specific towards T. congolense relative to the mammalian cells. Additionally, the in vivo study revealed that the imidazoles exhibited promising anti-Trypanosoma efficacy corroborating the in vitro anti-parasite capacity. In particular, three imidazole compounds (C1, C6, and C8) not only cleared the systemic parasite burden but cured infected rats after no death was recorded. On the other hand, the remaining five imidazole compounds (C2, C3, C4, C5, and C7) drastically reduced the systemic parasite load while extending survival time of the infected rats by 14 days as compared with control. Untreated control died 3 days post-infection, while the rats treated with diminazene aceturate were cured comparable to the results obtained for C1, C6, and C8. In conclusion, this is the first study demonstrating the potential of these new series of imidazoles to clear the systemic parasite burden in infected rats. Furthermore, a high selectivity index of imidazoles towards T. congolense in vitro and the oral LD50 in rats support anti-parasite specific action. Together, findings support the anti-parasitic prospects of the new series of imidazole derivatives.

    Original languageEnglish
    Pages (from-to)199-207
    Number of pages9
    JournalYale Journal of Biology and Medicine
    Volume94
    Issue number2
    Publication statusPublished - 2021 Jun

    Keywords

    • Chemotherapy
    • Drug discovery
    • Infectious Diseases
    • Medicinal biochemistry
    • Medicinal chemistry
    • Trypanosomiasis

    ASJC Scopus subject areas

    • Biochemistry, Genetics and Molecular Biology(all)

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