Browsing School of Pharmacy by Author "Malan, Sarel F."
Now showing items 1-7 of 7
-
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 ... -
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 ... -
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, ...