Browsing by Author "Joubert, Jacques"
Now showing items 1-17 of 17
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Antimycobacterial Activity, Synergism, and Mechanism of Action Evaluation of Novel Polycyclic Amines against Mycobacterium tuberculosis
Kapp, Erika; Joubert, Jacques; Sampson, Samantha, L; Malan, Sarel, F; Sharma, Rajan; Warner, Digby, F; Seldon, Ronnett; Jordaan, Audrey; de Vos, Margaretha (Advances in Pharmacological and Pharmaceutical Sciences, 2021-06)Mycobacterium tuberculosis has developed extensive resistance to numerous antimycobacterial agents used in the treatment of tuberculosis. Insufficient intracellular accumulation of active moieties allows for selective ... -
Common defciencies found in generic Finished Pharmaceutical Product (FPP) applications submitted for registration to the South African Health Products Regulatory Authority (SAHPRA)
Moeti, Lerato; Litedu, Madira; Joubert, Jacques (Springer Nature, 2022)The aim of the study was to investigate the common defciencies observed in the Finished Pharmaceutical Product (FPP) section of generic product applications submitted to SAHPRA. The study was conducted retrospectively ... -
Common Deficiencies Found in the Active Pharmaceutical Ingredient (API) Section of Non-sterile Generic Products Submitted for Registration by SAHPRA
Moeti, Lerato; Joubert, Jacques (Springer Science and Business Media Deutschland GmbH, 2023)Purpose: This research study aims to determine the qualitative and quantitative common deficiencies included in the API section of dossiers submitted to SAHPRA. The study was conducted retrospectively over a 7-year period ... -
Crystal structure, Hirshfeld surface analysis and DFT studies of 5-(adamantan-1-yl)-3-[(4- chlorobenzyl)sulfanyl]-4-methyl4H-1,2,4-triazole, a potential 11βHSD1 inhibitor
Joubert, Jacques; Al-Wahaibi, Lamya; Blacque, Olivier (Scientific Reports, 2019)5-(Adamantan-1-yl)-3-[(4-chlorobenzyl)sulfanyl]-4-methyl-4H-1,2,4-triazole (4) was identifed as a potential 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor and this paper describes the in-depth structural ... -
Crystal structure, hirshfeld surface analysis and dft studies of 5-(adamantan-1-yl)-3-[(4-chlorobenzyl)sulfanyl]-4-methyl-4h-1,2,4-triazole, a potential 11β-hsd1 inhibitor
Joubert, Jacques (Scientific Reports, 2019)5-(Adamantan-1-yl)-3-[(4-chlorobenzyl)sulfanyl]-4-methyl-4H-1,2,4-triazole (4) was identified as a potential 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor and this paper describes the in-depth structural ... -
Discovery of 9-phenylacridinediones as highly selective butyrylcholinesterase inhibitors through structure-based virtual screening
Joubert, Jacques; Kapp, Erika (Elsevier, 2020)Butyrylcholinesterase (BuChE) is considered a promising drug target as it plays an important role in the pro-gression of late stage Alzheimer’s disease (AD). Two compound libraries were selected and 64 124 aminecontaining ... -
The implementation of a risk based assessment approach by the South African Health pProducts Regulatory Authority (SAHPRA)
Moeti, Lerato; Litedu, Madira; Joubert, Jacques (Springer, 2023)An extensive backlog of pending regulatory decisions is one of the major historical challenges that the South African Health Products Regulatory Authority (SAHPRA) inherited from the Medicine Control Council (MCC). Revising ... -
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 ... -
Regulatory registration timelines of generic medicines in South Africa: Assessment of the performance of SAHPRA between 2011 and 2022
Moeti, Lerato; Litedu, Madira; Joubert, Jacques (Springer, 2023)Various regulatory authorities are experiencing backlogs of applications which result in delayed access to medicines for patients. The objective of this study is to critically assess the registration process utilised by ... -
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 ... -
Structural analysis, molecular modelling and preliminary competition bnding studies of AM-DAN as a NMDA Receptor PCP-Site Fluorescent Ligand
Ndzibongwana, Sethu; Ngobese, Samukelo; Sayed, Ahmad; Shongwe, Ciniso; White-Phillips, Simon; Joubert, Jacques (MDPI, 2019)Excitotoxicity related to the dysfunction of the N-methyl-d-aspartate receptor (NMDAR) has been indicated to play an integral role in the pathophysiology of multiple disease states, including neurodegenerative disorders ... -
Structural Insights and Docking Analysis of Adamantane-Linked 1,2,4-Triazole Derivatives as Potential 11 -HSD1 Inhibitors
Osman, Doaa, A; Macias, Mario, A; Zondagh, Luke, S; Joubert, Jacques; Al- Wahaibi, Lamya, H; Al- Shaalan, Nora, H; Garcia- Granda, Santiago; El-Emam, Ali, A (Molecules, 2021)The solid-state structural analysis and docking studies of three adamantane-linked 1,2,4- triazole derivatives are presented. Crystal structure analyses revealed that compound 2 crystallizes in the triclinic P-1 space ... -
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 (Arkivoc, 2020-09)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, ... -
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 (Arkivoc, 2020-09)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, ... -
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, ...