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Synthesis and pharmacological evaluation of novel tacrine derivatives as potential acetylcholinesterase inhibitors

Authorized Users Only
2021
Authors
Jevtić, Ivana
Penjišević, Jelena
Kostić-Rajačić, Slađana
Conference object (Published version)
Metadata
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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 inhibitors
Source:
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
Publisher:
  • The Société de Chimie Thérapeutique (SCT) / French Medicinal Chemistry Society
Funding / projects:
  • Ministry of Education, Science and Technological Development, Republic of Serbia, Grant no. 200026 (University of Belgrade, Institute of Chemistry, Technology and Metallurgy - IChTM) (RS-200026)
[ Google Scholar ]
Handle
https://hdl.handle.net/21.15107/rcub_cer_5837
URI
https://cer.ihtm.bg.ac.rs/handle/123456789/5837
Collections
  • Radovi istraživača / Researchers' publications
Institution/Community
IHTM
TY  - 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 .

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