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Synthesis and In Vitro Antiprotozoan Evaluation of 4-/8-Aminoquinoline-based Lactams and Tetrazoles

Molecules (Basel, Switzerland), 2020-12, Vol.25 (24), p.5941

2020

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Including African data in drug discovery and development

Nature reviews. Drug discovery, 2023-07, Vol.22 (7), p.521-522

2023

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Recent Approaches to Chemical Discovery and Development Against Malaria and the Neglected Tropical Diseases Human African Trypanosomiasis and Schistosomiasis

Chemical reviews, 2014-11, Vol.114 (22), p.11138-11163

2014

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Total Synthesis of the Antimycobacterial Natural Product Chlorflavonin and Analogs via a Late-Stage Ruthenium(II)-Catalyzed ortho-C(sp2)-H-Hydroxylation

Pharmaceuticals (Basel, Switzerland), 2022-08, Vol.15 (8), p.984

2022

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Intestinal Transport Characteristics and Metabolism of C-Glucosyl Dihydrochalcone, Aspalathin

Molecules (Basel, Switzerland), 2017-03, Vol.22 (4), p.554

2017

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Differences in the metabolism of fusidic acid in man and mice

Drug metabolism and pharmacokinetics, 2017-01, Vol.32 (1), p.S47-S48

2017

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Early metabolic profiling of pyrido[1,2-a]benzimidazoles in mouse liver microsomes by LC-MS/MS

Drug metabolism and pharmacokinetics, 2017-01, Vol.32 (1), p.S48-S48

2017

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AI can help to tailor drugs for Africa - but Africans should lead the way

Nature (London), 2024-04, Vol.628 (8007), p.265-267

2024

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Defining the Determinants of Specificity of Plasmodium Proteasome Inhibitors

Journal of the American Chemical Society, 2018-09, Vol.140 (36), p.11424-11437

2018

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Synthesis and structure–activity-relationship studies of thiazolidinediones as antiplasmodial inhibitors of the Plasmodium falciparum cysteine protease falcipain-2

European journal of medicinal chemistry, 2015-01, Vol.90, p.507-518

2015

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Spiropyrimidinetriones: a Class of DNA Gyrase Inhibitors with Activity against Mycobacterium tuberculosis and without Cross-Resistance to Fluoroquinolones

Antimicrobial agents and chemotherapy, 2022-04, Vol.66 (4), p.e0219221-e0219221

2022

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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

Journal of medicinal chemistry, 2021-04, Vol.64 (8), p.5198-5215

2021

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Novel 3‑Trifluoromethyl-1,2,4-oxadiazole Analogues of Astemizole with Multi-stage Antiplasmodium Activity and In Vivo Efficacy in a Plasmodium berghei Mouse Malaria Infection Model

Journal of medicinal chemistry, 2022-12, Vol.65 (24), p.16695-16715

2022

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Synthesis and biological evaluation of 2-aminothiazole derivatives as antimycobacterial and antiplasmodial agents

Bioorganic & medicinal chemistry letters, 2014-01, Vol.24 (2), p.560-564

2014

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Identification, Characterization, and Optimization of 2,8-Disubstituted-1,5-naphthyridines as Novel Plasmodium falciparum Phosphatidylinositol-4-kinase Inhibitors with in Vivo Efficacy in a Humanized Mouse Model of Malaria

Journal of medicinal chemistry, 2018-07, Vol.61 (13), p.5692-5703

2018

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Azaaurones as Potent Antimycobacterial Agents Active against MDR‐ and XDR‐TB

ChemMedChem, 2019-08, Vol.14 (16), p.1537-1546

2019

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Synthesis and biological characterisation of ester and amide derivatives of fusidic acid as antiplasmodial agents

Bioorganic & medicinal chemistry letters, 2017-02, Vol.27 (3), p.658-661

2017

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UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria

Antimicrobial agents and chemotherapy, 2018-09, Vol.62 (9)

2018

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Pyrrolo[3,4‑c]pyridine-1,3(2H)‑diones: A Novel Antimycobacterial Class Targeting Mycobacterial Respiration

Journal of medicinal chemistry, 2015-12, Vol.58 (23), p.9371-9381

2015

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Antimalarial Imidazopyridines Incorporating an Intramolecular Hydrogen Bonding Motif: Medicinal Chemistry and Mechanistic Studies

ACS infectious diseases, 2023-04, Vol.9 (4), p.928-942

2023

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2,8-Disubstituted-1,5-naphthyridines as Dual Inhibitors of Plasmodium falciparum Phosphatidylinositol-4-kinase and Hemozoin Formation with In Vivo Efficacy

Journal of medicinal chemistry, 2024-07, Vol.67 (13), p.11401-11420

2024

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1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in Mycobacterium tuberculosis

Journal of medicinal chemistry, 2021-09, Vol.64 (17), p.12790-12807

2021

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Antimalarial Pyrido[1,2‑a]benzimidazoles: Lead Optimization, Parasite Life Cycle Stage Profile, Mechanistic Evaluation, Killing Kinetics, and in Vivo Oral Efficacy in a Mouse Model

Journal of medicinal chemistry, 2017-02, Vol.60 (4), p.1432-1448

2017

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Antimalarial Pyrido[1,2‑a]benzimidazole Derivatives with Mannich Base Side Chains: Synthesis, Pharmacological Evaluation, and Reactive Metabolite Trapping Studies

ACS infectious diseases, 2019-03, Vol.5 (3), p.372-384

2019

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Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and In Vivo Efficacy in the Plasmodium falciparum NSG Mouse Model

Journal of medicinal chemistry, 2020-11, Vol.63 (21), p.13013-13030

2020

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Synthesis and In Vitro Antiprotozoan Evaluation of 4-/8-Aminoquinoline-based Lactams and Tetrazoles

Including African data in drug discovery and development

Recent Approaches to Chemical Discovery and Development Against Malaria and the Neglected Tropical Diseases Human African Trypanosomiasis and Schistosomiasis

Total Synthesis of the Antimycobacterial Natural Product Chlorflavonin and Analogs via a Late-Stage Ruthenium(II)-Catalyzed ortho-C(sp2)-H-Hydroxylation

Intestinal Transport Characteristics and Metabolism of C-Glucosyl Dihydrochalcone, Aspalathin

Differences in the metabolism of fusidic acid in man and mice

Early metabolic profiling of pyrido[1,2-a]benzimidazoles in mouse liver microsomes by LC-MS/MS

AI can help to tailor drugs for Africa - but Africans should lead the way

Defining the Determinants of Specificity of Plasmodium Proteasome Inhibitors

Synthesis and structure–activity-relationship studies of thiazolidinediones as antiplasmodial inhibitors of the Plasmodium falciparum cysteine protease falcipain-2

Spiropyrimidinetriones: a Class of DNA Gyrase Inhibitors with Activity against Mycobacterium tuberculosis and without Cross-Resistance to Fluoroquinolones

Antimalarial Benzimidazole Derivatives Incorporating Phenolic Mannich Base Side Chains Inhibit Microtubule and Hemozoin Formation: Structure–Activity Relationship and In Vivo Oral Efficacy Studies

Novel 3‑Trifluoromethyl-1,2,4-oxadiazole Analogues of Astemizole with Multi-stage Antiplasmodium Activity and In Vivo Efficacy in a Plasmodium berghei Mouse Malaria Infection Model

Synthesis and biological evaluation of 2-aminothiazole derivatives as antimycobacterial and antiplasmodial agents

Identification, Characterization, and Optimization of 2,8-Disubstituted-1,5-naphthyridines as Novel Plasmodium falciparum Phosphatidylinositol-4-kinase Inhibitors with in Vivo Efficacy in a Humanized Mouse Model of Malaria

Azaaurones as Potent Antimycobacterial Agents Active against MDR‐ and XDR‐TB

Synthesis and biological characterisation of ester and amide derivatives of fusidic acid as antiplasmodial agents

UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria

Pyrrolo[3,4‑c]pyridine-1,3(2H)‑diones: A Novel Antimycobacterial Class Targeting Mycobacterial Respiration

Antimalarial Imidazopyridines Incorporating an Intramolecular Hydrogen Bonding Motif: Medicinal Chemistry and Mechanistic Studies

2,8-Disubstituted-1,5-naphthyridines as Dual Inhibitors of Plasmodium falciparum Phosphatidylinositol-4-kinase and Hemozoin Formation with In Vivo Efficacy

1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in Mycobacterium tuberculosis

Antimalarial Pyrido[1,2‑a]benzimidazoles: Lead Optimization, Parasite Life Cycle Stage Profile, Mechanistic Evaluation, Killing Kinetics, and in Vivo Oral Efficacy in a Mouse Model

Antimalarial Pyrido[1,2‑a]benzimidazole Derivatives with Mannich Base Side Chains: Synthesis, Pharmacological Evaluation, and Reactive Metabolite Trapping Studies

Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and In Vivo Efficacy in the Plasmodium falciparum NSG Mouse Model

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