Browsing by Author "Malan, Sarel F."
Now showing items 1-10 of 10
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3D-QSAR and docking studies of pentacycloundecylamines at the sigma-1 (σ1) receptor
Geldenhuys, Werner J.; Novotny, Nicholas; Malan, Sarel F.; Van der Schyf, Cornelis J. (Elsevier, 2013)Pentacycloundecylamine (PCU) derived compounds have been shown to be promising lead structures for the development of novel drug candidates aimed at a variety of neurodegenerative and psychiatric diseases. Here we show for ... -
4-oxatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives as nmda receptor- And VGCC blockers with neuroprotective potential
Egunlusi, Ayodeji O.; Malan, Sarel F.; Omoruyi, Sylvester Ifeanyi (MPDI, 2020)The impact of excitotoxicity mediated by N-methyl-D-aspartate (NMDA) receptor overactivation and voltage gated calcium channel (VGCC) depolarization is prominent among the postulated processes involved in the development ... -
Exploration of scaffolds from natural products with antiplasmodial activities, currently registered antimalarial drugs and public malarial screen data
Egieyeh, Samuel; Syce, James; Christoffels, Alan; Malan, Sarel F. (MDPI, 2016)In light of current resistance to antimalarial drugs, there is a need to discover new classes of antimalarial agents with unique mechanisms of action. Identification of unique scaffolds from natural products with in vitro ... -
Microwave-assisted methods for the synthesis of pentacyclo[5.4.0.02,6.03,10.05,9]undecylamines
Joubert, Jacques; Sharma, Rajan; Onani, Martin O.; Malan, Sarel F. (Elsevier, 2013)Efficient methodologies for the preparation of pentacyclo[5..4.0.02,6.03,10.05,9]undecane (PCU) amine derivatives are described via microwave-assisted synthesis. The obtained results revealed that microwave-assisted synthetic ... -
Multi-targeted directed ligands for Alzheimer’s disease: design of novel lead coumarin conjugates
Repsold, B.P.; Malan, Sarel F.; Joubert, Jacques; Oliver, D.W. (Taylor & Francis, 2018)Alzheimer’s Disease (AD) is a neurodegenerative disease characterized by central nervous system insults with progressive cognitive (memory, attention) and non-cognitive (anxiety, depression) impairments. Pathophysiological ... -
Predictive classifier models built from natural products with antimalarial bioactivity using machine learning approach
Egieyeh, Samuel; Syce, James; Malan, Sarel F.; Christoffels, Alan (Public Library of Science, 2018)In view of the vast number of natural products with potential antiplasmodial bioactivity and cost of conducting antiplasmodial bioactivity assays, it may be judicious to learn from previous antiplasmodial bioassays and ... -
Prioritization of anti-malarial hits from nature: Chemo-informatic profiling of natural products with in vitro antiplasmodial activities and currently registered anti-malarial drugs
Egieyeh, Samuel Ayodele; Syce, James; Malan, Sarel F. (BMC, 2016)A large number of natural products have shown in vitro antiplasmodial activities. Early identification and prioritization of these natural products with potential for novel mechanism of action, desirable pharmacokinetics ... -
Small molecule efflux pump inhibitors in Mycobacterium tuberculosis: a rational drug design perspective
Kapp, Erika; Malan, Sarel F.; Joubert, Jacques; Sampson, Samantha L. (Bentham Science Publishers, 2018)Drug resistance in Mycobacterium tuberculosis (M. tuberculosis) complicates management of tuberculosis. Efflux pumps contribute to low level resistance and acquisition of additional high level resistance mutations through ... -
Synthesis and biological evaluations of NO-donating oxa- and aza-pentacycloundecane derivatives as potential neuroprotective candidates
Sharma, Rajan; Joubert, Jacques; Malan, Sarel F. (MDPI, 2018)In order to utilize the neuroprotective properties of polycyclic cage compounds, and explore the NO-donating ability of nitrophenyl groups, an array of compounds was synthesized where the different nitrophenyl groups ... -
Synthesis of 4-oxatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives as lead scaffolds for neuroprotective agents
Egunlusi, Ayodeji O.; Malan, Sarel F.; Joubert, Jacques (Arkat USA, 2020)Neurodegenerative disorders are characterised by progressive loss of neuronal functions. Of the proposed mechanisms, excitotoxicity, mediated by prolonged glutamate activation and calcium overload, is prominent. NGP1-01, ...