Synthesis of Novel Quinolinecarboxamide Derivatives with Estrogenic Activity.

Um, Soo‐Jong; Park, Si-Ho; Park, Chong‐Ho; Chang, Byung‐Ha; Yoon, Jeong‐Hyeok; Sin, Hong‐Sig

doi:10.1002/chin.200343126

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“…2-(4-benzylpiperidin-1-ylmethyl)-5-(Bocaminopentyloxy)-indan-1-one (15) Yield 45 %. IR (KBr) cm − 1 : 736, 1 675, 1 710, 2 739, 2 957, 3 268.…”

Section: General Procedures For Synthesis Of Compounds (14) and (15)mentioning

confidence: 99%

“…Based on our study, we determined 2 methods for synthesizing compounds with a variable length of the carbon chain at C-5. N-Boc-aminoethoxy derivatives 10, 11 were used to perform O-alkylation of 5, 6 with N-Boc-2-bromoethylamine 7 using potassium carbonate in refl uxing acetonitrile [ 15 ] . Similar reaction conditions employing N-Boc-3-bromopropylamine 8, led to the desired 12, 13 ( • ▶ Fig.…”

Section: ▼ Chemistrymentioning

confidence: 99%

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Synthesis and Biological Activity of New Donepezil-Hydrazinonicotinamide Hybrids

2013

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Synthesis and Biological Activity of New Donepezil-Hydrazinonicotinamide Hybrids decreased level of choline acetyltransferase, leading to impaired synthesis and uptake of acetylcholine (ACh) neurotransmitter [ 3 , 4 ] . As ACh is degraded by cholinesterase, it stands to reason that cholinergic transmission can be improved by inhibiting the activity of this enzyme. 2 kinds of choline esterases catalyzing hydrolysis of choline esters exist in the central nervous system: acetylcholinesterase (AChE), the so-called true esterase, and butyrylcholinesterase (BChE), referred to as pseudocholinesterase or non-specifi c cholinesterase. AChE is bound to the membrane of cholinergic neurons, whereas BChE is present both in the neurons and in the glial cells. Both enzymes show 65 % homology, and the main diff erences pertain to their substrate specifi city. Acetylcholinesterase selectively and rapidly hydrolyzes acetylcholine in cholinergic synapses. In turn, butyrylcholinesterase can also hydrolyze butyrylcholine and some medications and drugs, aside from acetylcholine. Moreover, it regulates cholinergic transmission in states of acetylcholinesterase defi ciency. In healthy individuals, AChE accounts for 80 % of esterase activity within the central nervous system, whereas the remaining 20 % is provided by BChE. In Alzheimer's disease, the activity of AChE can be reduced to 67 % of normal level in certain brain regions; simultaneously, an Introduction ▼ Alzheimer's disease (AD) is a slow progressive, degenerative disorder of the CNS. It is the most common form of dementia accounting for about 50-60 % of all cases of dementia among persons over 65 years of age. Currently, an estimated 4.5 million older people suff er with Alzheimer's disease (AD), and researchers predict that by 2 050 the number could nearly triple, to 13.5 million [ 1 ] . This disease is important not only because of the number of aff ected patients but also because it leads to signifi cant physical and emotional burden on families and caregivers. Alzheimer's disease is characterized by the loss of memory and learning ability, together with a reduced ability to perform basic activities of daily living. AD patients exhibit marked neuropsychiatric symptoms such as apathy, irritability, anxiety, depression, hallucinations and verbal and physical agitation [ 2 ] . Studies performed during the last 20 years revealed that disordered cholinergic transmission is behind cognitive impairment present in Alzheimer's disease patients. The disorders in transmission result from the reduced number of cholinergic neurons in brain regions associated with higher cognitive functions, i. e. in the neocortex and hippocampus, as well as from the Abstract ▼Currently available treatment used in Alzheimer's disease is based on acetylcholinesterase inhibitors, e. g. donepezil, tacrine, galantamine, and rivastigmine. In the present study some derivatives of donepezil were synthesized, and their potential anticholinesterase properties were investigated using the colorimetric Ellman's m...

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“…2-(4-benzylpiperidin-1-ylmethyl)-5-(Bocaminopentyloxy)-indan-1-one (15) Yield 45 %. IR (KBr) cm − 1 : 736, 1 675, 1 710, 2 739, 2 957, 3 268.…”

Section: General Procedures For Synthesis Of Compounds (14) and (15)mentioning

confidence: 99%

Section: ▼ Chemistrymentioning

confidence: 99%

Synthesis and Biological Activity of New Donepezil-Hydrazinonicotinamide Hybrids

2013

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Synthesis of Novel Quinolinecarboxamide Derivatives with Estrogenic Activity.

Abstract: Some novel quinolinecarboxamide derivatives like (VI) and (VIII) are synthesized and tested as potential nonsteroidal estrogenic compounds. -(UM, S.-J.; PARK, S.-H.; PARK, C.-H.; CHANG, B.-H.; YOON, J.-H.; SIN, H.-S.; Bull. Korean Chem.

Cited by 1 publication

References 8 publications

Synthesis and Biological Activity of New Donepezil-Hydrazinonicotinamide Hybrids

Synthesis and Biological Activity of New Donepezil-Hydrazinonicotinamide Hybrids

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Synthesis of Novel Quinolinecarboxamide Derivatives with Estrogenic Activity.

Abstract: Some novel quinolinecarboxamide derivatives like (VI) and (VIII) are synthesized and tested as potential nonsteroidal estrogenic compounds. -(UM, S.-J.; PARK*, S.-H.; PARK, C.-H.; CHANG, B.-H.; YOON, J.-H.; SIN*, H.-S.; Bull. Korean Chem.

Cited by 1 publication

References 8 publications

Synthesis and Biological Activity of New Donepezil-Hydrazinonicotinamide Hybrids

Synthesis and Biological Activity of New Donepezil-Hydrazinonicotinamide Hybrids

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Abstract: Some novel quinolinecarboxamide derivatives like (VI) and (VIII) are synthesized and tested as potential nonsteroidal estrogenic compounds. -(UM, S.-J.; PARK, S.-H.; PARK, C.-H.; CHANG, B.-H.; YOON, J.-H.; SIN, H.-S.; Bull. Korean Chem.