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DC Field | Value | Language |
---|---|---|
dc.contributor.author | Mahesh, R. | - |
dc.date.accessioned | 2023-11-20T08:44:20Z | - |
dc.date.available | 2023-11-20T08:44:20Z | - |
dc.date.issued | 2017-10 | - |
dc.identifier.uri | https://www.sciencedirect.com/science/article/abs/pii/S0968089617313408 | - |
dc.identifier.uri | http://dspace.bits-pilani.ac.in:8080/xmlui/handle/123456789/13180 | - |
dc.description.abstract | The prokaryotic ATP-dependent ClpP protease, localized in the relict plastid of malaria parasite, represents a potential drug target. In the present study, we utilized in silico structure-based screening and medicinal chemistry approaches to identify a novel pyrimidine series of compounds inhibiting P. falciparum ClpP protease activity and evaluated their antiparasitic activities. Structure-activity relationship indicated that morpholine moiety at C2, an aromatic substitution at N3 and a 4-oxo moiety on the pyrimidine are important for potent inhibition of ClpP enzyme along with antiparasiticidal activity. Compound 33 exhibited potent antiparasitic activity (EC₅₀ 9.0 ± 0.2 μM), a 9-fold improvement over the antiparasitic activity of the hit molecule 6. Treatment of blood stage P. falciparum cultures with compound 33 caused morphological and developmental abnormalities in the parasites; further, compound 33 treatment hindered apicoplast development indicating the targeting of apicoplast. | en_US |
dc.language.iso | en | en_US |
dc.publisher | Elsevier | en_US |
dc.subject | Pharmacy | en_US |
dc.subject | ATP-dependent ClpP protease | en_US |
dc.subject | Plasmodial ClpP | en_US |
dc.subject | Apicoplast | en_US |
dc.title | A novel class of Plasmodial ClpP protease inhibitors as potential antimalarial agents | en_US |
dc.type | Article | en_US |
Appears in Collections: | Department of Pharmacy |
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