Search Results - "Dziwornu, Godwin"
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Discovery of Novel Cyclic Ethers with Synergistic Antiplasmodial Activity in Combination with Valinomycin
Published in Molecules (Basel, Switzerland) (10-12-2021)“…With drug resistance threatening our first line antimalarial treatments, novel chemotherapeutics need to be developed. Ionophores have garnered interest as…”
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Synthesis and Evaluation of Chalcone-Quinoline Based Molecular Hybrids as Potential Anti-Malarial Agents
Published in Molecules (Basel, Switzerland) (05-07-2021)“…Molecular hybridization is a drug discovery strategy that involves the rational design of new chemical entities by the fusion (usually via a covalent linker)…”
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Antimicrobial and in silico studies of the triterpenoids of Dichapetalum albidum
Published in Heliyon (01-07-2023)“…Here we report a new polyhydroxylated triterpene, 2β,6β,21α-trihydroxyfriedelan-3-one (4) isolated from the root and stem bark of Dichapetalum albidum A. Chev…”
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Isolation, Characterization and Antiproliferative Activity of New Metabolites from the South African Endemic Red Algal Species Laurencia alfredensis
Published in Molecules (Basel, Switzerland) (23-03-2017)“…The marine red algae of the genus have been widely studied for their structurally diverse and biologically active secondary metabolites. We report here the…”
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Cytotoxic activity of marine sponge extracts from the sub-Antarctic Islands and the Southern Ocean
Published in South African Journal of Science (01-11-2016)“…Over the past 50 years, marine invertebrates, especially sponges, have proven to be a valuable source of new and/or bioactive natural products that have the…”
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Novel antimycobacterial C-21 amide derivatives of the antibiotic fusidic acid: synthesis, pharmacological evaluation and rationalization of media-dependent activity using molecular docking studies in the binding site of human serum albumin
Published in MedChemComm (01-06-2019)“…Fusidic acid is a natural product antibiotic used clinically, primarily against staphylococcal infections. It has also exhibited antimycobacterial activity…”
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Constituents of the Roots of Dichapetalum pallidum and Their Anti-Proliferative Activity
Published in Molecules (Basel, Switzerland) (27-03-2017)“…As part of our search for bioactive compounds from the Dichapetalaceae, repeated chromatographic purification of the roots of a hitherto unexamined species, ,…”
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New dihydroxycucurbitacin D's from the Namib desert endemic plant Acanthosicyos horridus (!nara)
Published in Fitoterapia (01-11-2021)“…Acanthosicyos horridus Welw. ex Hook.f. (!nara) is a leafless, thorny, melon-producing plant endemic to the hyper-arid Namib Desert. The methanol crude extract…”
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Plasmepsin Inhibitors in Antimalarial Drug Discovery: Medicinal Chemistry and Target Validation (2000 to Present)
Published in Journal of medicinal chemistry (14-05-2020)“…Plasmepsins represent novel antimalarial drug targets. However, plasmepsin-based antimalarial drug discovery efforts in the past 2 decades have generally…”
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The dichapetalins and dichapetalin-type compounds: structural diversity, bioactivity, and future research perspectives
Published in Natural product reports (17-10-2024)“…Covering mainly from 2013 up to 2023 with relevant references to work done before 2013First reported in 1995, the dichapetalins and analogous compounds…”
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The implication of Mycobacterium tuberculosis-mediated metabolism of targeted xenobiotics
Published in Nature reviews. Chemistry (01-05-2023)“…Drug metabolism is generally associated with liver enzymes. However, in the case of Mycobacterium tuberculosis ( Mtb ), the causative agent of tuberculosis…”
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Structure-activity relationship analyses of fusidic acid derivatives highlight crucial role of the C-21 carboxylic acid moiety to its anti-mycobacterial activity
Published in Bioorganic & medicinal chemistry (01-07-2020)“…[Display omitted] Fusidic acid (FA) is a potent congener of the fusidane triterpenoid class of antibiotics. Structure-activity relationship (SAR) studies…”
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Rv0684/fusA1, an Essential Gene, Is the Target of Fusidic Acid and Its Derivatives in Mycobacterium tuberculosis
Published in ACS infectious diseases (13-08-2021)“…Tuberculosis (TB), caused by Mycobacterium tuberculosis, is a major global health concern given the increase in multiple forms of drug-resistant TB. This…”
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Another decade of antimalarial drug discovery: New targets, tools and molecules
Published in Progress in medicinal chemistry (2024)“…Malaria remains a devastating but preventable infectious disease that disproportionately affects the African continent. Emerging resistance to current…”
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Chemotherapy for human schistosomiasis: how far have we come? What's new? Where do we go from here?
Published in RSC medicinal chemistry (01-04-2020)“…Globally, schistosomiasis threatens more than 700 million lives, mostly children, in poor localities of tropical and sub-tropical areas with morbidity due to…”
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Antimalarial Benzimidazole Derivatives Incorporating Phenolic Mannich Base Side Chains Inhibit Microtubule and Hemozoin Formation: Structure–Activity Relationship and In Vivo Oral Efficacy Studies
Published in Journal of medicinal chemistry (22-04-2021)“…A novel series of antimalarial benzimidazole derivatives incorporating phenolic Mannich base side chains at the C2 position, which possess dual asexual blood…”
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Novel antimycobacterial C-21 amide derivatives of the antibiotic fusidic acid: synthesis, pharmacological evaluation and rationalization of media-dependent activity using molecular docking studies in the binding site of human serum albumin† †Electronic supplementary information (ESI) available. See DOI: 10.1039/c9md00161a
Published in MedChemComm (18-04-2019)“…Fusidic acid is a natural product antibiotic used clinically, primarily against staphylococcal infections. Fusidic acid is a natural product antibiotic used…”
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18
2,8-Disubstituted-1,5-naphthyridines as Dual Inhibitors of Plasmodium falciparum Phosphatidylinositol-4-kinase and Hemozoin Formation with In Vivo Efficacy
Published in Journal of medicinal chemistry (11-07-2024)“…Structure–activity relationship studies of 2,8-disubstituted-1,5-naphthyridines, previously reported as potent inhibitors of Plasmodium falciparum (Pf)…”
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Antimalarial Pyrido[1,2‑a]benzimidazole Derivatives with Mannich Base Side Chains: Synthesis, Pharmacological Evaluation, and Reactive Metabolite Trapping Studies
Published in ACS infectious diseases (08-03-2019)“…A novel series of pyrido[1,2-a]benzimidazoles bearing Mannich base side chains and their metabolites were synthesized and evaluated for in…”
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Pharmacokinetics and Organ Distribution of C‑3 Alkyl Esters as Potential Antimycobacterial Prodrugs of Fusidic Acid
Published in ACS infectious diseases (13-03-2020)“…Fusidic acid (FA) has previously been shown to be rapidly metabolized in rodents to its C-3 epimer, which has significantly lower antimycobacterial activity…”
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