Synthesis and pharmacological evaluation of novel tacrine derivatives as potential acetylcholinesterase inhibitors
Abstract
Alzheimer's disease (AD) is a progressive, neurodegenerative disorder characterized by deterioration of
cognitive skills and it is the most abundant form of dementia according to the World Health Organization
(WHO).1 Tacrine belongs to a class of acetylcholinesterase inhibitors (AChEIs) and it was formerly used in the
treatment of AD symptoms. Albeit no longer in clinical use due to its hepatotoxicity, tacrine ring system is
extensively investigated as pharmacophore in novel AChEIs, many of which showed improved pharmacological
profile in the preclinical studies.2 Here we present optimized synthetic pathway and pharmacological evaluation
of three novel tacrine derivatives (5, 6 and 7), possessing functionalized piperidine connected with tacrine via
five methylene groups alkyl chain
Keywords:
Alzheimer's disease / Tacrine / acetylcholinesterase inhibitorsSource:
Book of abstracts - 56th International conference on medicinal chemistry, RICT 2021, "Interfacing chemical biology and drug discovery", July 7-9, 2021, virtual event, 2021, 119-119Publisher:
- The Société de Chimie Thérapeutique (SCT) / French Medicinal Chemistry Society
Funding / projects:
Collections
Institution/Community
IHTMTY - CONF AU - Jevtić, Ivana AU - Penjišević, Jelena AU - Kostić-Rajačić, Slađana PY - 2021 UR - https://cer.ihtm.bg.ac.rs/handle/123456789/5837 AB - Alzheimer's disease (AD) is a progressive, neurodegenerative disorder characterized by deterioration of cognitive skills and it is the most abundant form of dementia according to the World Health Organization (WHO).1 Tacrine belongs to a class of acetylcholinesterase inhibitors (AChEIs) and it was formerly used in the treatment of AD symptoms. Albeit no longer in clinical use due to its hepatotoxicity, tacrine ring system is extensively investigated as pharmacophore in novel AChEIs, many of which showed improved pharmacological profile in the preclinical studies.2 Here we present optimized synthetic pathway and pharmacological evaluation of three novel tacrine derivatives (5, 6 and 7), possessing functionalized piperidine connected with tacrine via five methylene groups alkyl chain PB - The Société de Chimie Thérapeutique (SCT) / French Medicinal Chemistry Society C3 - Book of abstracts - 56th International conference on medicinal chemistry, RICT 2021, "Interfacing chemical biology and drug discovery", July 7-9, 2021, virtual event T1 - Synthesis and pharmacological evaluation of novel tacrine derivatives as potential acetylcholinesterase inhibitors SP - 119 EP - 119 UR - https://hdl.handle.net/21.15107/rcub_cer_5837 ER -
@conference{ author = "Jevtić, Ivana and Penjišević, Jelena and Kostić-Rajačić, Slađana", year = "2021", abstract = "Alzheimer's disease (AD) is a progressive, neurodegenerative disorder characterized by deterioration of cognitive skills and it is the most abundant form of dementia according to the World Health Organization (WHO).1 Tacrine belongs to a class of acetylcholinesterase inhibitors (AChEIs) and it was formerly used in the treatment of AD symptoms. Albeit no longer in clinical use due to its hepatotoxicity, tacrine ring system is extensively investigated as pharmacophore in novel AChEIs, many of which showed improved pharmacological profile in the preclinical studies.2 Here we present optimized synthetic pathway and pharmacological evaluation of three novel tacrine derivatives (5, 6 and 7), possessing functionalized piperidine connected with tacrine via five methylene groups alkyl chain", publisher = "The Société de Chimie Thérapeutique (SCT) / French Medicinal Chemistry Society", journal = "Book of abstracts - 56th International conference on medicinal chemistry, RICT 2021, "Interfacing chemical biology and drug discovery", July 7-9, 2021, virtual event", title = "Synthesis and pharmacological evaluation of novel tacrine derivatives as potential acetylcholinesterase inhibitors", pages = "119-119", url = "https://hdl.handle.net/21.15107/rcub_cer_5837" }
Jevtić, I., Penjišević, J.,& Kostić-Rajačić, S.. (2021). Synthesis and pharmacological evaluation of novel tacrine derivatives as potential acetylcholinesterase inhibitors. in Book of abstracts - 56th International conference on medicinal chemistry, RICT 2021, "Interfacing chemical biology and drug discovery", July 7-9, 2021, virtual event The Société de Chimie Thérapeutique (SCT) / French Medicinal Chemistry Society., 119-119. https://hdl.handle.net/21.15107/rcub_cer_5837
Jevtić I, Penjišević J, Kostić-Rajačić S. Synthesis and pharmacological evaluation of novel tacrine derivatives as potential acetylcholinesterase inhibitors. in Book of abstracts - 56th International conference on medicinal chemistry, RICT 2021, "Interfacing chemical biology and drug discovery", July 7-9, 2021, virtual event. 2021;:119-119. https://hdl.handle.net/21.15107/rcub_cer_5837 .
Jevtić, Ivana, Penjišević, Jelena, Kostić-Rajačić, Slađana, "Synthesis and pharmacological evaluation of novel tacrine derivatives as potential acetylcholinesterase inhibitors" in Book of abstracts - 56th International conference on medicinal chemistry, RICT 2021, "Interfacing chemical biology and drug discovery", July 7-9, 2021, virtual event (2021):119-119, https://hdl.handle.net/21.15107/rcub_cer_5837 .