In pursuit of new anti-malarial candidates: novel synthesized and characterized pyrano-benzodioxepin analogues attenuated Plasmodium berghei replication in malaria-infected mice

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dc.contributor.authorAtolani O
dc.contributor.authorSulaiman FA
dc.contributor.authorHamid AA
dc.contributor.authorAlayo A
dc.contributor.authorAkina AC
dc.contributor.authorOloriegbe S
dc.contributor.authorBalogun BA
dc.contributor.authorOlatunji GA
dc.contributor.authorKambizi L
dc.date.accessioned2022-07-26T11:50:18Z
dc.date.available2022-07-26T11:50:18Z
dc.date.issued2021
dc.descriptionHeliyon
dc.description.abstractMalaria, a parasitic disease, is one of the major causes of morbidity and mortality, particularly in the tropics. Following the increased resistance of the primary causative parasite, Plasmodium sp, to the mainstream drug, artemisinin combination therapies (ACTs), combating malaria incidences, morbidity and mortality have remained elusive. Novel pyrano-benzodioxepin derivatives (DHA-PABA and DHA-LEVO) were synthesized and characterized using Fourier transform infrared (FT-IR) and nuclear magnetic resonance (NMR) spectroscopies. The compounds were subjected to standard in vivo antimalarial screening (using chloroquine-sensitive strain) in mice, and the toxicity was also determined using a standard assay. The observed elevation in serum alkaline phosphatase and acid phosphatase activity in the untreated and the group administered lower doses of DHA-LEVO is an indication of the hepatic stage of the parasite in the experimental animal, which is accompanied by significant perturbation in the membrane of the hepatocyte leading to leakage of this enzyme out of the liver cells. The semisynthetic pyrano-benzodioxepin derivatives act rapidly by clearing the parasite load from the blood. The novel pyrano-benzodioxepin candidates containing endoperoxide functionality hold promise in the pursuit of new monotherapy drug candidates against the virulent strain of the plasmodium.
dc.identifier.citation10.1016/j.heliyon.2021.e08517
dc.identifier.issn2405-8440
dc.identifier.urihttps://nerd.ethesis.ng/handle/123456789/255
dc.language.isoen
dc.subjectArtemisinin
dc.subjectAminobenzoic acid
dc.subjectAnti-malarial
dc.subjectPyrano-benzodioxepin
dc.subjectChemosuppression
dc.titleIn pursuit of new anti-malarial candidates: novel synthesized and characterized pyrano-benzodioxepin analogues attenuated Plasmodium berghei replication in malaria-infected mice
dc.typeArticle
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