Synthesis and acetylcholinesterase(AChE) inhibitory activity of some N-substituted-5-chloro-2(3H)-benzoxazolone derivatives

Soyer, Zeynep

doi:10.12991/201317387

Cited by 9 publications

(7 citation statements)

References 12 publications

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“…60) derived from secondary aliphatic amines or primary arylamines, and bis-Mannich bases 314 derived either from primary aliphatic amines (X ¼ NR, R ¼ C 2 H 5 , R 1 C 6 H 4 CH 2 CH 2 , R 1 ¼ H, 4-Cl, 3,4-(CH 3 O) 2 ) or piperazine have been evaluated for AChE inhibitory activity using Ellman's method. The degree of inhibition was in the range of 70e82% at a concentration of 1 mM, but decreased to 8e34% at 0.1 mM, whereas the degree of AChE inhibition by tacrine was virtually the same at both concentrations (greater than 99%) [466].…”

Section: Inhibitors Of Cholinesterasesmentioning

confidence: 87%

Mannich bases in medicinal chemistry and drug design

Roman¹

2015

European Journal of Medicinal Chemistry

281

110

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The biological activity of Mannich bases, a structurally heterogeneous class of chemical compounds that are generated from various substrates through the introduction of an aminomethyl function by means of the Mannich reaction, is surveyed, with emphasis on the relationship between structure and biological activity. The review covers extensively the literature reports that have disclosed Mannich bases as anticancer and cytotoxic agents, or compounds with potential antibacterial and antifungal activity in the last decade. The most relevant studies on the activity of Mannich bases as antimycobacterial agents, antimalarials, or antiviral candidates have been included as well. The review contains also a thorough coverage of anticonvulsant, anti-inflammatory, analgesic and antioxidant activities of Mannich bases. In addition, several minor biological activities of Mannich bases, such as their ability to regulate blood pressure or inhibit platelet aggregation, their antiparasitic and anti-ulcer effects, as well as their use as agents for the treatment of mental disorders have been presented. The review gives in the end a brief overview of the potential of Mannich bases as inhibitors of various enzymes or ligands for several receptors.

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Section: Inhibitors Of Cholinesterasesmentioning

confidence: 87%

Mannich bases in medicinal chemistry and drug design

Roman¹

2015

European Journal of Medicinal Chemistry

281

110

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“…A series N-substituted-5-chloro-2(3H)-benzoxazolone derivatives were synthesized and evaluated by [1] their acetylcholinesterase inhibitory activity. These compounds were synthesized by Mannich reaction of 5-chloro-2(3H)-benzoxazolone with the appropriated amines.…”

Section: Introductionmentioning

confidence: 99%

Crystal Structure and Theoretical Study of N,N-di[(5-chloro-2-oxo-2,3-dihydrobenzo[d]oxazole-3-yl)methyl]ethanamine

Aydın¹,

Soyer²,

Akkurt³

et al. 2017

ujpa

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The aim of the present work is to explore crystal and electronic structure ofIn the title compound, C 18 H 15 Cl 2 N 3 O 4 , the two 2, 3-dihydro-1, 3-benzoxazole ring systems are almost planar and make a dihedral angle of 96.12(7) with each other. The ethyl group is disordered over two set of sites with a site-occupancy ratio of 0.766(12):0.234(12). The crystal structure contain intermolecular C-H...O hydrogen bonds which form a zigzag chains along the c-axis, C-H...π interactions and π-π stacking interactions [centroid-centroid distance = 3.5668(19) Å].

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“…Approaches to enhance cholinergic function in AD have included stimulation of cholinergic receptors or prolonging the availability of ACh released into the neuronal synaptic cleft by use of agents which restore 383 the level of acetylcholine through inhibition of both AChE and BChE. Since ancient times phytochemicals have been used in traditional cultures to restore and declining cognitive functions lost with neurodegenerative diseases [2] . Currently, only four acetylcholinesterase inhibitors namely, tacrine, donepezil, rivastigmine and galantamine have been approved by the US Food and Drug Administration [3] . Thus, the development of effective new agents as acetylcholinesterase inhibitors is needed.…”

Section: Introductionmentioning

confidence: 99%