Synthesis and pharmacology evaluation of novel 1-benzyl-n-(4-(4-arylpiperazin-1-yl)phenyl)piperidin-4-carboxamides, as potential acetylcholinesterase inhibitors
Abstract
Alzheimer’s disease (AD) is a neurodegenerative disease which affects over 50 milion people worldwide.1) AD
mainly affects people ages 65 and above. Symptoms are memory loss, decline in learning capacity, and language
problems. One of currently available treatments for Alzheimer's disease consists of Cholinesterase (ChEIs)
inhibitors, which raise acetylcholine levels in the brain. The drugs currently approved by the FDA for this
purpose are donepezil, rivastigmine and galantamine.
As a part of our research we designed and synthesized seven novel compounds (6a-g) as potential
acetylcholinesterase inhibitors (AChEIs). The compounds contain N-benzyl piperidine moiety, which is common
in many inhibitors including donepezil,2) and N-aryl piperazine moieties.
Keywords:
Alzheimer’s disease / Cholinesterase inhibitors / acetylcholine / acetylcholinesterase inhibitors / N-benzyl piperidine / N-aryl piperazineSource:
Book of Abstracts - 26th EFMC-ISMC, International Symposium on Medicinal Chemistry, Aug. 29-Sept. 2, 2021, virtual event, 2021, 413-413Publisher:
- Division of Medicinal Chemistry and Chemical Biology of the Swiss Chemical Society
- European Federation for Medicinal Chemistry and Chemical Biology (EFMC)
Funding / projects:
- Ministry of Science, Technological Development and Innovation of the Republic of Serbia, institutional funding - 200026 (University of Belgrade, Institute of Chemistry, Technology and Metallurgy - IChTM) (RS-MESTD-inst-2020-200026)
Collections
Institution/Community
IHTMTY - CONF AU - Krunić, Mihajlo AU - Penjišević, Jelena AU - Jevtić, Ivana AU - Ivanović, Milovan AU - Kostić-Rajačić, Slađana PY - 2021 UR - https://cer.ihtm.bg.ac.rs/handle/123456789/5843 AB - Alzheimer’s disease (AD) is a neurodegenerative disease which affects over 50 milion people worldwide.1) AD mainly affects people ages 65 and above. Symptoms are memory loss, decline in learning capacity, and language problems. One of currently available treatments for Alzheimer's disease consists of Cholinesterase (ChEIs) inhibitors, which raise acetylcholine levels in the brain. The drugs currently approved by the FDA for this purpose are donepezil, rivastigmine and galantamine. As a part of our research we designed and synthesized seven novel compounds (6a-g) as potential acetylcholinesterase inhibitors (AChEIs). The compounds contain N-benzyl piperidine moiety, which is common in many inhibitors including donepezil,2) and N-aryl piperazine moieties. PB - Division of Medicinal Chemistry and Chemical Biology of the Swiss Chemical Society PB - European Federation for Medicinal Chemistry and Chemical Biology (EFMC) C3 - Book of Abstracts - 26th EFMC-ISMC, International Symposium on Medicinal Chemistry, Aug. 29-Sept. 2, 2021, virtual event T1 - Synthesis and pharmacology evaluation of novel 1-benzyl-n-(4-(4-arylpiperazin-1-yl)phenyl)piperidin-4-carboxamides, as potential acetylcholinesterase inhibitors SP - 413 EP - 413 UR - https://hdl.handle.net/21.15107/rcub_cer_5843 ER -
@conference{ author = "Krunić, Mihajlo and Penjišević, Jelena and Jevtić, Ivana and Ivanović, Milovan and Kostić-Rajačić, Slađana", year = "2021", abstract = "Alzheimer’s disease (AD) is a neurodegenerative disease which affects over 50 milion people worldwide.1) AD mainly affects people ages 65 and above. Symptoms are memory loss, decline in learning capacity, and language problems. One of currently available treatments for Alzheimer's disease consists of Cholinesterase (ChEIs) inhibitors, which raise acetylcholine levels in the brain. The drugs currently approved by the FDA for this purpose are donepezil, rivastigmine and galantamine. As a part of our research we designed and synthesized seven novel compounds (6a-g) as potential acetylcholinesterase inhibitors (AChEIs). The compounds contain N-benzyl piperidine moiety, which is common in many inhibitors including donepezil,2) and N-aryl piperazine moieties.", publisher = "Division of Medicinal Chemistry and Chemical Biology of the Swiss Chemical Society, European Federation for Medicinal Chemistry and Chemical Biology (EFMC)", journal = "Book of Abstracts - 26th EFMC-ISMC, International Symposium on Medicinal Chemistry, Aug. 29-Sept. 2, 2021, virtual event", title = "Synthesis and pharmacology evaluation of novel 1-benzyl-n-(4-(4-arylpiperazin-1-yl)phenyl)piperidin-4-carboxamides, as potential acetylcholinesterase inhibitors", pages = "413-413", url = "https://hdl.handle.net/21.15107/rcub_cer_5843" }
Krunić, M., Penjišević, J., Jevtić, I., Ivanović, M.,& Kostić-Rajačić, S.. (2021). Synthesis and pharmacology evaluation of novel 1-benzyl-n-(4-(4-arylpiperazin-1-yl)phenyl)piperidin-4-carboxamides, as potential acetylcholinesterase inhibitors. in Book of Abstracts - 26th EFMC-ISMC, International Symposium on Medicinal Chemistry, Aug. 29-Sept. 2, 2021, virtual event Division of Medicinal Chemistry and Chemical Biology of the Swiss Chemical Society., 413-413. https://hdl.handle.net/21.15107/rcub_cer_5843
Krunić M, Penjišević J, Jevtić I, Ivanović M, Kostić-Rajačić S. Synthesis and pharmacology evaluation of novel 1-benzyl-n-(4-(4-arylpiperazin-1-yl)phenyl)piperidin-4-carboxamides, as potential acetylcholinesterase inhibitors. in Book of Abstracts - 26th EFMC-ISMC, International Symposium on Medicinal Chemistry, Aug. 29-Sept. 2, 2021, virtual event. 2021;:413-413. https://hdl.handle.net/21.15107/rcub_cer_5843 .
Krunić, Mihajlo, Penjišević, Jelena, Jevtić, Ivana, Ivanović, Milovan, Kostić-Rajačić, Slađana, "Synthesis and pharmacology evaluation of novel 1-benzyl-n-(4-(4-arylpiperazin-1-yl)phenyl)piperidin-4-carboxamides, as potential acetylcholinesterase inhibitors" in Book of Abstracts - 26th EFMC-ISMC, International Symposium on Medicinal Chemistry, Aug. 29-Sept. 2, 2021, virtual event (2021):413-413, https://hdl.handle.net/21.15107/rcub_cer_5843 .