A5082654448- Synthesis and biological activity
- Synthesis and Biological Evaluation
- HIV/AIDS drug development and treatment
- Computational Drug Discovery Methods
- Parkinson's Disease Mechanisms and Treatments
- Malaria Research and Control
- Phenothiazines and Benzothiazines Synthesis and Activities
- Cyclopropane Reaction Mechanisms
- Trypanosoma species research and implications
- Synthesis and Characterization of Heterocyclic Compounds
- Chemical Synthesis and Analysis
- Innovative Microfluidic and Catalytic Techniques Innovation
- Adenosine and Purinergic Signaling
- Click Chemistry and Applications
- Cholinesterase and Neurodegenerative Diseases
- Electrochemical sensors and biosensors
- Iron Metabolism and Disorders
- Drug Solubulity and Delivery Systems
- Advanced Drug Delivery Systems
- Synthesis and Reactivity of Heterocycles
- Drug-Induced Hepatotoxicity and Protection
- Research on Leishmaniasis Studies
- Radiopharmaceutical Chemistry and Applications
- Carbohydrate Chemistry and Synthesis
- Bone health and osteoporosis research
North-West University
2010-2024
Abstract The treatment of neuropsychiatric and neurodegenerative disorders such as depression Parkinson’s disease represent significant challenges in healthcare. Enzymes that metabolise neurotransmitter amines are important drug targets for these inhibitors enzymes have played key roles therapeutic agents. For example, monoamine oxidase (MAO) A been used decades antidepressant agents act by inhibiting the central metabolism serotonin noradrenaline, while MAO-B conserve dopamine supply to...
The small molecule, isatin, is a well-known reversible inhibitor of the monoamine oxidase (MAO) enzymes with IC50 values 12.3 and 4.86 μM for MAO-A MAO-B, respectively. While interaction isatin MAO-B has been characterized, only few studies have explored structure-activity relationships (SARs) MAO inhibition by analogues. current study therefore evaluated series 14 analogues as in vitro inhibitors human MAO-B. results indicated good potency some five compounds exhibiting < 1 μM....
The aim of this study was to synthesize a series mono-, di- and trisubstituted derivatives the human African trypanosomiasis drug eflornithine (alpha-difluoromethylornithine, DMFO, CAS 70052-12-9) determine their partition coefficients, assess whether they deliver parent in plasma. If increased plasma concentrations could be achieved way, an oral dosage form would possible. derivatives, nine total, were successfully synthesized by multi-step derivatisation on either its alpha-carboxylic...
The aim of this study was to determine the in vitro antibacterial activity nitrocatechol chalcone and pyrazoline derivatives previously synthesised by our research group against Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii aerogenes, create validate a pharmacophore model using data. enrichment factor (EF10%) area under receiver operating characteristic (ROC-AUC) curve were used model. Using validated novel designed synthesised, whereafter these also determined...
Abstract Neurodegenerative disorders are caused by the progressive death of neuronal cells in specific regions brain and spinal cord. The most common neurodegenerative Alzheimer’s disease Parkinson’s disease. inhibition enzymes that metabolise neurotransmitter amines is an important approach treatment these monoamine oxidase (MAO) B inhibitors have thus been used for Inhibitors MAO-A isoform, turn, clinically affective (e.g., major depression) anxiety disorders. Recent studies shown...
Background: Methylene blue and some of its analogues have known antibacterial activity, however their exact mechanism action is unknown Objective: In this study, the minimum inhibitory concentration (MIC) bactericidal (MBC) several methylene were determined against five bacterial strains, whereafter data used to create validate a pharmacophore model. Methods: The agar dilution method was screen for while broth microdilution determine MIC MBC. A model constructed validated using rank score,...
Background: Novel antibiotics are needed to stem the rise of antimicrobial resistance. N-Methyl-2-phenylmaleimide (NMP) compounds previously synthesised by our research group structural analogues 2,3,5-substituted perhydropyrrolo[3,4-d]isoxazole-4,6-diones found others have antibacterial activity. Objectives: This study aims explain significance NMPs and their The activity was determined against Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii,...
Antimicrobial resistance has rendered the sulfonamide class of antibiotics obsolete. An additional binding site on dihydropteroate synthase (DHPS) enzyme, i.e., pterin site, been shown to be a valid alternative well-known para-aminobenzoic acid site. The aim this study was identify compounds that may bind using computational approach. Different computer docking/scoring combinations were firstly validated root mean square deviation, enrichment factor (EF10%) and area under receiver operating...