3-Hydroxpyridin-4-one prodrugs as novel antimalarials

Fakorede, Foluke; Liu, Z. D.; Hider, Robert C.

doi:10.1111/j.2042-7158.1998.tb02313.x

Cited by 1 publication

(2 citation statements)

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“…160 The prodrug concept can be utilized to overcome the disadvantage of poor oral absorption and hydrophilicity, such as CP38 ester prodrugs which can facilitate the transport of CP38 to the blood supply. 161 In order to improve the efficiency of the antimalaria activity of HPOs, nitrogen centers were introduced to HPOs in order to target acidic vacuoles, such as those found in the parasite. Compounds 101 and 102 were found to be the most promising candidates, with appropriate LogP values to facilitate their penetration into intracellular organelles while being sufficiently hydrophilic to lack the general toxicity.…”

Section: Hpo-glucosidesmentioning

confidence: 99%

“…These HPOs can inhibit malaria both in vitro and in vivo . The prodrug concept can be utilized to overcome the disadvantage of poor oral absorption and hydrophilicity, such as CP38 ester prodrugs which can facilitate the transport of CP38 to the blood supply . In order to improve the efficiency of the antimalaria activity of HPOs, nitrogen centers were introduced to HPOs in order to target acidic vacuoles, such as those found in the parasite.…”

Section: Pharmacological Applications Of Hydroxypyridinone Derivativesmentioning

confidence: 99%

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Hydroxypyridinone-Based Iron Chelators with Broad-Ranging Biological Activities

et al. 2020

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Iron plays an essential role in all living cells because of its unique chemical properties. It is also the most abundant trace element in mammals. However, when iron is present in excess or inappropriately located, it becomes toxic. Excess iron can become involved in free radical formation, resulting in oxidative stress and cellular damage. Iron chelators are used to treat serious pathological disorders associated with systemic iron overload. Hydroxypyridinones stand out for their outstanding chelation properties, including high selectivity for Fe 3+ in the biological environment, ease of derivatization, and good biocompatibility. Herein, we overview the potential for multifunctional hydroxypyridinone-based chelators to be used as therapeutic agents against a wide range of diseases associated either with systemic or local elevated iron levels.

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Section: Hpo-glucosidesmentioning

confidence: 99%

Section: Pharmacological Applications Of Hydroxypyridinone Derivativesmentioning

confidence: 99%