Structural and inhibition studies of thiamine monosphosphate kinase from Mycobacterium tuberculosis

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Biochemical and structural characterization of novel drug targets regulating polyamine biosynthesis in the human malaria parasite, Plasmodium falciparum

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Screening of natural compounds inhibiting biofilm formation by antibiotic resistant enterobacteria using experimental trials and computational molecular modelling

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Identification of bioactive ingredients from Cleome gynandra and the physicochemical study of their microencapsulation in beta-cyclodextrin

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Mechanism of Action Studies of Phenotypic Whole-cell Active Antimalarial Leads Through Target Identification by Korkor, Constance

“…To mitigate the limitations of resolution, Airyscan and super-resolution structured-illumination microscopy (SR-SIM) were employed. …”
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Machine learning approaches towards identifying inhibitors for plasmodium falciparum cGMP-dependent protein kinase. by Thibaud, Jessica Leigh

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Design of Selective Plasmodium falciparum Kinase Inhibitors using Computer-Aided Drug Discovery by Kamunya, Stephanie Gathoni

“…Using structure-based drug design methods, several strategies were used to design potent dual PfPI4K/PfPKG inhibitors with reduced activity against human kinases specifically mTOR and human type III beta phosphatidylinositol-4 kinase (HuPI4KIIIβ). …”
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Isolation of antiplasmodial naphthylisoquinoline alkaloids from Ancistrocladus sp. through bioassay-guided fractionation

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Synthesis, physicochemical and biological evaluation of N-dealkylated metabolites of antimalarial pyrido[1,2-a]benzimidazoles and related compounds containing a Mannich base side-c... by Ferger, Richard

“…The benzimidazole scaffold is an extensively researched privileged scaffold in medicinal chemistry because of its capacity to interact with numerous biological systems in various diseases, including malaria. Based on previous metabolite identification studies in liver microsomes, a new series of pyrido[1,2-a]benzimidazole (PBI) metabolites containing Mannich base side-chains were designed and synthesized. …”
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Anti-inflammatory and anti-diabetic properties of plant extracts and compounds from Scabiosa columbaria and Sclerocarya birrea

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Modulation of virulence factors in biofilm-forming Klebsiella pneumoniae via selected South African medicinal plants and phytochemical compounds

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Antimalarial benzimidazoles and related structures incorporating an intramolecular hydrogen bonding motif: medicinal chemistry and mechanistic studies by Attram, Henrietta Dede

“…In essence, these observations support hemozoin inhibition as a mechanism of action of compound 1.3 while pointing to other targets within the parasite based on widespread association with other organelles. …”
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Characterization and biological activity of antifungal compounds present in Breonadia salicina (Rubiaceae) leaves

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Antimicrobial and antimalarial activity of Tabernaemontana elegans Stapf. (Apocynaceae)

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Elucidation of the mode of action of a furanone based antituberculosis compound by Ngwane, Andile Happyboy

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Design, synthesis, and structure-activity relationship studies of dual Plasmodium falciparum phosphatidylinositol 4-kinase and cGMP-dependent protein kinase inhibitors by Gachuhi, Samuel Njoroge

“…In this study, an in silico-guided structural modification strategy was undertaken towards optimizing dual Plasmodium kinase inhibition and anti-plasmodium activity while also mitigating potency against its oncological human target, mTOR and off-target PI4KIIIb (Figure 1). …”
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Antimalarial imidazopyridazines and aminopyrazines: synthesis, physicochemical optimization and structure-activity relationships by Cheuka, Peter Mubanga

“…Further medicinal chemistry optimization led to identification of other derivatives which, albeit exhibiting complete cure of P. berghei-infected mice, still displayed poor solubility and hERG inhibition issues. …”
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Controlling Haemonchus contortus using bioactive compounds from plants with antifungal activity

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Clinically relevant mutations contributing to drug resistance in Mycobacterium tuberculosis by Du Plessis, Juanelle

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Proteomic characterisation of primary breast tumour extracellular matrix

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