Design and synthesis of tacrine-ferulic acid hybrids as multi-potent anti-Alzheimer drug candidates

Bioorganic & Medicinal Chemistry Letters
Lei FangMichael Decker

Abstract

Five tacrine-ferulic acid hybrids (6a-e) were designed and synthesized as multi-potent anti-Alzheimer drug candidates. All target compounds have better acetylcholinesterase inhibitory activity and comparable butyrylcholinesterase inhibitory activity in relation to tacrine. Interestingly, 6d showed a reversible and non-competitive inhibitory action for acetylcholinesterase indicating interaction with the peripheral anionic site, whereas a reversible but competitive inhibitory action for butyrylcholinesterase. The antioxidant study revealed that four target compounds have, compared to Trolox, high ability to absorb reactive oxygen species.

References

Jul 3, 1998·Alzheimer Disease and Associated Disorders·S I GraconD Kraemer
Jan 8, 2004·Journal of Agricultural and Food Chemistry·Alberto DávalosBegoña Bartolomé
Feb 20, 2007·Mini Reviews in Medicinal Chemistry·Quan LiuGeorge Perry

❮ Previous
Next ❯

Citations

Dec 18, 2013·Journal of Computer-aided Molecular Design·Sawsan AbuhamdahMutasem O Taha
Feb 26, 2013·Archives of Pharmacal Research·Preet Anand, Baldev Singh
Mar 29, 2013·Bioorganic & Medicinal Chemistry·Todd J EckroatSylvie Garneau-Tsodikova
May 17, 2013·Chemical Research in Toxicology·Mario Esquivias-PérezMaría Jesús Oset-Gasque
Sep 6, 2012·International Journal of Molecular Sciences·Paweł SzymańskiElżbieta Mikiciuk-Olasik
Dec 19, 2012·Mitochondrion·Sofia BenfeitoFernanda Borges
Mar 25, 2014·European Journal of Medicinal Chemistry·Tamás KálaiKálmán Hideg
Jan 15, 2015·Future Medicinal Chemistry·Mohamed BenchekrounJosé Marco-Contelles
Sep 4, 2015·Molecular Diversity·Manjinder SinghOm Silakari
Jul 28, 2011·Medicinal Research Reviews·Rafael LeónJosé Marco-Contelles
Jul 9, 2009·Phytotherapy Research : PTR·María C CarpinellaSara M Palacios
Nov 19, 2013·The Journal of Pharmacy and Pharmacology·Katharina ZengerBirgit Kraus
Mar 31, 2016·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Houssem BoulebdJosé Marco-Contelles
Aug 19, 2016·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Mike JonesJohn F Gilmer
Aug 6, 2015·European Journal of Medicinal Chemistry·Belma Zengin KurtSalvatore Guccione
Jul 28, 2012·Journal of Ethnopharmacology·Emmanuel Adekanmi AdewusiVanessa Steenkamp
Nov 27, 2014·Journal of Computer-aided Molecular Design·Katarina NikolicJohn B O Mitchell
May 14, 2016·Chemico-biological Interactions·Luana G de SouzaJose D Figueroa-Villar
May 10, 2016·Expert Opinion on Drug Delivery·Ibrahim A AljuffaliJia-You Fang
May 18, 2016·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Youssef DgachiLhassane Ismaili
Jul 10, 2016·European Journal of Medicinal Chemistry·Marco Antonio CeschiLaurent Emmanuel Dardenne
Oct 12, 2016·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Yingbo FuXueshi Huang
Oct 25, 2016·Future Medicinal Chemistry·M Amélia SantosSílvia Chaves
Jan 31, 2017·Journal of Enzyme Inhibition and Medicinal Chemistry·Wen-Yu WuJin-Ao Duan
Feb 26, 2015·Brazilian Journal of Medical and Biological Research = Revista Brasileira De Pesquisas Médicas E Biológicas·A S N FormagioJ E Carvalho
May 10, 2017·Future Medicinal Chemistry·Houssem BoulebdAli Belfaitah
May 10, 2017·Future Medicinal Chemistry·Sandra GuneschMichael Decker
Apr 28, 2017·International Journal of Molecular Sciences·Jucilene Silva AraújoLeticia M Estevinho

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.