Design, and facile synthesis of 1,3 diaryl-3-(arylamino)propan-1-one derivatives as the potential alpha-amylase inhibitors and antioxidants

Bashary, Roqia; Khatik, Gopal L.

doi:10.1016/j.bioorg.2018.10.010

Cited by 45 publications

(21 citation statements)

References 30 publications

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“…For this molecular modeling software, Autodock-vina [28,29,30] was used by the pdb or protein selected 4MS3 as a GABA (gamma-aminobutyric acid) receptor of (human) due to the unavailability of nematode GABA protein crystal structure and were downloaded from the protein data bank. The GABA receptor is a well-known target for piperazine exhibits weak GABA-mimetic and causes reversible paralysis of body wall muscle [31,32,33].…”

Section: Molecular Docking Studiesmentioning

confidence: 99%

In vitro anthelmintic activity of Chenopodium album and in-silico prediction of mechanistic role on Eisenia foetida

Choudhary

Khatik

Choudhary³

et al. 2021

Heliyon

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Helminths born diseases are related to pitiable management practices and improper control strategies. The medicinal plants contain various phytoconstituents that are liable for their anthelmintic activity. The aerial parts of the Chenopodium album were successively extracted with microwaves assisted extraction using petroleum ether, ethyl acetate, methanol, hydroalcoholic and aqueous solvents to get respective extracts (CAPE, CAEE, CAME, CAHE, and CAAE). All the extracts were analyzed for preliminary phytochemical screening for the identification of phytoconstituents. The anthelmintic activity was analyzed on Indian adult earthworms Eisenia foetida using piperazine citrate (PCT) as a standard drug. All the extracts (apart from CAAE) lead to paralysis and fatality of the earthworms. CAEE extract exhibits highly significant anthelmintic activity at a 10 mg/ml concentration by causing paralysis and fatality of earthworms and was more potent than PCT suspension. At a concentration of 10 mg/ml, paralysis and death time for CAEE was recorded as (10.08 ± 1.11) and (65.28 ± 2.09) respectively, while for standard piperazine citrate, it was recorded as (22.96 ± 1.12) and (65.09 ± 1.23). The CAEE exhibits two major compounds by LC-MS, i.e., NG and DG, that are mainly accountable for the Chenopodium album anthelmintic activity . The plant possesses GABA-mimetic action and thereby leads to flaccid, reversible paralysis of the body wall muscle.

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Section: Molecular Docking Studiesmentioning

confidence: 99%

In vitro anthelmintic activity of Chenopodium album and in-silico prediction of mechanistic role on Eisenia foetida

Choudhary

Khatik

Choudhary³

et al. 2021

Heliyon

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“…Inhibition of α -amylase by the crude extracts Iodine-starch test was conducted, to test the plants ability to inhibit α -amylase enzyme. This was done according to the method developed by Bashary and Khatik (2019). The procedure depends on the formation of a blue or violet complex when iron reacts with starch acarbose that was used as a standard.…”

Section: Frapð%þ ¼mentioning

confidence: 99%

Phytochemical screening, anti-oxidant activity and α-amylase inhibition study using different extracts of loquat (Eriobotrya japonica) leaves

Mogole

Omwoyo

Mtunzi

2020

Heliyon

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Diabetes Mellitus is an endocrine disorder which causes insulin deficiency. Medicinal plants are documented to be efficacious in the management of the disease. The current research set to determine the phytochemicals present, anti-oxidant activity and investigate the potency of Eriobotrya japonica against α-amylase inhibition. The leaves of the plant were extracted sequentially. The different extracts were evaluated for the presence of phytochemicals and their potential anti-oxidant and α-amylase inhibition activity. Methanol with the highest polarity, gave the highest yield of 20% and hexane with the lowest polarity have the lowest yield of 2.09%. This trend resembled that observed for the total flavanoid and total phenolic content analysis which gave values of 0.3822 mg QAE/mg and 3.810 mg GAE/mg respectively for methanolic and hexane extracts. The extracts of methanol recorded higher DPPH free radical scavenging activity of 87% and gave the lowest IC 50 of 0.5336 which was below that of ascorbic acid used as a control. Hexane extract had a higher α-amylase inhibitory activity of 24% at 1 μg/ml as compared to other extracts. Generally hexane extracts of Eriobotrya japonica exhibits mild inhibitory activity against α-amylase enzyme which is recommended than the conventional therapy which maximally inhibits the enzyme causing major side effects. The results obtained herein support the use of the plant as an anti-diabetic agent at higher concentrations.

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“…22 Employing aldol condensation to form chalcones (7a-7j) was initially attempted following by established protocols, specifically using NaOH in EtOH at room temperature overnight. [23][24] The diarylated chalcone synthesis worked well (data not included). However, synthesis using heteroaryl aldehydes (eg.…”

Section: Chemistrymentioning

confidence: 99%

Novel Furan-2-yl-1H-pyrazoles Possess Inhibitory Activity against α-Synuclein Aggregation

Ryan

Jahan

et al. 2020

ACS Chem. Neurosci.

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A series of novel furan-2-yl-1H-pyrazoles and their chemical precursors were synthesised and evaluated for their effectiveness at disrupting α-synuclein (α-syn) aggregation in vitro. The compounds were found to inhibit α-syn aggregation with efficacy comparable to the promising drug candidate anle138b. The results of this study indicate that compounds 8b, 8l and 9f may qualify as secondary leads for the structure-activity relationship studies aimed to identify the suitable compounds for improving the modulatory activity targeted at α-syn self-assembly related to Parkinson's disease.

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Design, and facile synthesis of 1,3 diaryl-3-(arylamino)propan-1-one derivatives as the potential alpha-amylase inhibitors and antioxidants

Cited by 45 publications

References 30 publications

In vitro anthelmintic activity of Chenopodium album and in-silico prediction of mechanistic role on Eisenia foetida

In vitro anthelmintic activity of Chenopodium album and in-silico prediction of mechanistic role on Eisenia foetida

Phytochemical screening, anti-oxidant activity and α-amylase inhibition study using different extracts of loquat (Eriobotrya japonica) leaves

Novel Furan-2-yl-1H-pyrazoles Possess Inhibitory Activity against α-Synuclein Aggregation

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