Crystal Structure of the N Domain of Human Somatic Angiotensin I-converting Enzyme Provides a Structural Basis for Domain-specific Inhibitor Design

Hazel Corradi, Sylva L. U. Schwager, Aloysius T. Nchinda, +2

Journal of Molecular Biology

Molecular PharmacologyCrystal StructureBiochemistryBiomolecular Structure PredictionMedicine +8

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

Christel Brunschwig, Nina Lawrence, Dale Taylor, +45

Antimicrobial Agents and Chemotherapy

3,5-Diaryl-2-aminopyridines as a Novel Class of Orally Active Antimalarials Demonstrating Single Dose Cure in Mice and Clinical Candidate Potential

Yassir Younis, Frédèric Douelle, Tzu‐Shean Feng, +20

Journal of Medicinal Chemistry

Novel Orally Active Antimalarial Thiazoles

Diego González Cabrera, Frédèric Douelle, Tzu‐Shean Feng, +11

Journal of Medicinal Chemistry

Antiparasitic AgentMalariaCellular PharmacologyPharmacokineticsPre-clinical Pharmacology +16

Identification of a Potential Antimalarial Drug Candidate from a Series of 2-Aminopyrazines by Optimization of Aqueous Solubility and Potency across the Parasite Life Cycle

Claire Le Manach, Aloysius T. Nchinda, Tanya Paquet, +25

Journal of Medicinal Chemistry

Structure–Activity-Relationship Studies around the 2-Amino Group and Pyridine Core of Antimalarial 3,5-Diarylaminopyridines Lead to a Novel Series of Pyrazine Analogues with Oral in Vivo Activity

Yassir Younis, Frédèric Douelle, Diego González Cabrera, +13

Journal of Medicinal Chemistry

Pyridine CoreAntiparasitic AgentMalariaAntimalarial 3,5-Diarylaminopyridines LeadPharmacotherapy +15

Medicinal Chemistry Optimization of Antiplasmodial Imidazopyridazine Hits from High Throughput Screening of a SoftFocus Kinase Library: Part 1

Claire Le Manach, Diego González Cabrera, Frédèric Douelle, +15

Journal of Medicinal Chemistry

Pharmaceutical ScienceBioorganic ChemistryMedicinal Chemistry OptimizationPharmaceutical ChemistryPre-clinical Pharmacology +20

Novel Heterocyclic Analogues of the HIV‐1 Protease Inhibitor, Ritonavir

Perry T. Kaye, Musiliyu A. Musa, Aloysius T. Nchinda, +1

Synthetic Communications

Hiv‐1 Protease InhibitorMedicinal ChemistryProtease InhibitorBiochemistryMedicine +11

Synthesis of novel keto-ACE analogues as domain-selective angiotensin I-converting enzyme inhibitors

Aloysius T. Nchinda, Kelly Chibale, Pierre Redelinghuys, +1

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryNatural Product SynthesisBiochemistryMedicineNatural Sciences +6

Positional-Scanning Combinatorial Libraries of Fluorescence Resonance Energy Transfer Peptides for Defining Substrate Specificity of the Angiotensin I-Converting Enzyme and Development of Selective C-Domain Substrates

Patrícia Alessandra Bersanetti, Maria Claudina Camargo de Andrade, Dulce Elena Casarini, +5

Biochemistry

Bioorganic ChemistryPeptide EngineeringMolecular BiologyChemical BiologyProtein Folding +17