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Browsing by Impact Area "Pharmaceutical Technologies"

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Anti-mycobacterial peroxides: A new class of agents for development against tuberculosis

Author: Van der Westhuyzen, Christiaan W ; Haynes, J ; Panayides, Jenny-Lee ; Wiid, I ; Parkinson, C Date: 2020 Background: With few exceptions, existing tuberculosis drugs were developed many years ago and resistance profiles have emerged. This has created a need for new drugs with discrete modes of action. There is evidence that tuberculosis (like ... Read more
Assessing a sustainable manufacturing route to lapatinib

Author: Stark, RT ; Rye, DR ; Newton, OJ ; Deadman, BJ ; Miller, PW ; Panayides, Jenny-Lee ; Riley, Darren L ; Helldardt, K ; Hii, KK Date: Aug 2022 A synthetic route to an anti-cancer drug, lapatinib, was devised to support the development of a sustainable manufacturing process in South Africa. Quantitative metrics were employed to evaluate the sustainability of the key steps of the reaction. Read more
Binding pose analysis of hydroxyethylamine based ß-secretase inhibitors and application thereof to the design and synthesis of novel indeno[1,2-b]indole based inhibitors

Author: Van der Westhuizen, CJ ; Van Greunen, DG ; Cordier, W ; Nell, M ; Steenkamp, V ; Stander, A ; Panayides, Jenny-Lee ; Riley, DL Date: Nov 2020 ß-Secretase (BACE1) is recognised as a target for the treatment of Alzheimer’s disease, and transition-state isosteres such as hydroxyethylamines have shown promise when incorporated into BACE1 inhibitors. A computational investigation of ... Read more
A Cytotoxic Bis(1,2,3-triazol-5-ylidene)carbazolide Gold(III) complex targets DNA by partial intercalation

Author: Van der Westhuizen, D ; Slabber, CA ; Fernandes, MA ; Joubert, DF ; Kleinhans, G ; Van der Westhuizen, Carl J ; Stander, A ; Munro, OQ ; Bezuidenhout, DI Date: Jun 2021 The syntheses of bis(triazolium)carbazole precursors and their corresponding coinage metal (Au, Ag) complexes are reported. For alkylated triazolium salts, di- or tetranuclear complexes with bridging ligands were isolated, while the bis(aryl) ... Read more
Design and testing of an ozonolysis reactor module with on-the-fly ozone degassing under flow conditions

Author: Neyt, Nicole C ; Van der Westhuizen, Johan C ; Panayides, Jenny-Lee ; Riley, DL Date: Mar 2022 Ozonolysis is an attractive, efficient, and green means of introducing oxygen containing functionalities using only oxygen and electricity. Unfortunately, safety issues associated with the accumulation of dissolved ozone and potentially ... Read more
Discovery of novel Acetylcholinesterase inhibitors by virtual screening, in vitro screening, and molecular dynamics simulations

Author: Van van der Westhuizen, Johan C ; Stander, A ; Riley, DL ; Panayides, Jenny-Lee Date: Mar 2022 Alzheimer's disease is the most common neurodegenerative disease and currently poses a significant socioeconomic problem. This study describes the uses of computer-aided drug discovery techniques to identify novel inhibitors of acetylcholinesterase, ... Read more
Rapid formation of 2-lithio-1-(triphenylmethyl)imidazole and substitution reactions in flow†

Author: Wang, S ; Panayides, Jenny-Lee ; Riley, D ; Tighe, CJ ; Hii, KK Date: Sep 2021 The functionalisation of imidazoles is a necessary step in the formation of many active pharmaceutical intermediates. Herein, we report a flow chemistry approach for the rapid and efficient formation of 2-lithio-1-(triphenylmethyl)imidazole ... Read more
Riminophenazine derivatives as potential antituberculosis agents: Synthesis, biological, and electrochemical evaluations

Author: Bvumbi, Mpelegeng V ; Van der Westhuyzen, Christiaan W ; Mmutlane, EM ; Ngwane, A Date: Jul 2021 A series of novel riminophenazine derivatives, having ionizable alkyl substituents at N-5 and a variety of substituents on the C-3 imino nitrogen, at C-8 and on the pendant aryl group, have been designed and synthesized. Preliminary investigations ... Read more
Riminophenazine derivatives as potential antituberculosis agents: Synthesis, biological, and electrochemical evaluations

Author: Bvumbi, Mpelegeng V ; Van der Westhuyzen, Christiaan W ; Mmutlane, EM ; Ngwane, A Date: Jul 2021 A series of novel riminophenazine derivatives, having ionizable alkyl substituents at N-5 and a variety of substituents on the C-3 imino nitrogen, at C-8 and on the pendant aryl group, have been designed and synthesized. Preliminary investigations ... Read more
The synthesis of bupropion hydrochloride under greener and safer conditions utilizing flow technologies

Author: Van Wyk, LT ; Neyt, Nicole C ; Jugmohan, Jaimee ; Panayides, Jenny-Lee ; Riley, DL Date: Jan 2024 Globally, major depressive disorders are a leading cause of disconsolateness affecting more than 300 million individuals. Bupropion is a unique dopamine-norepinephrine reuptake inhibitor (DNRI) commonly utilized in the treatment of depression, ... Read more
Use of open-source software platform to develop dashboards for control and automation of flow chemistry equipment

Author: Van der Westhuizen, Johan ; Du Toit, Jurie H ; Neyt, Nicole C ; Riley, DL ; Panayides, Jenny-Lee Date: Jul 2022 We report the development of an open-source software approach to monitor and control flow chemistry reactors from any smart device utilising Node-RED which lowers the expertise required to expand the system further and automate other equipment. ... Read more

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Browsing by Impact Area "Pharmaceutical Technologies"

Browsing by Impact Area "Pharmaceutical Technologies"

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