Amide as a Potential Pharmacophore for Drug Designing of Novel Anticonvulsant Compounds

Kamal, Mehnaz; Jawaid, Talha; Dar, Umar Ali; Shah, Shakeel A.

doi:10.1002/9781119640929.ch11

Cited by 7 publications

(5 citation statements)

References 41 publications

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“…103,104 This is because amide bonds are a signicant part of many compounds including some important polymers, drugs, dyes, and agrochemical compounds. [105][106][107][108] Very recently, Wani et al employed sulfated starch as an efficient catalyst to transform the simple amines to their corresponding amides (Scheme 23). 109…”

Section: Synthesis Of Xanthene Compounds Containing Xanthene and Benz...mentioning

confidence: 99%

The untold story of starch as a catalyst for organic reactions

Sadeghi

2024

RSC Adv.

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Section: Synthesis Of Xanthene Compounds Containing Xanthene and Benz...mentioning

confidence: 99%

The untold story of starch as a catalyst for organic reactions

Sadeghi

2024

RSC Adv.

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“…Their ability to inhibit glutamate release, which impacts AMPA receptors, may shed light on their neuroprotective properties . Furthermore, these derivatives have demonstrated potential in realms like anti-Parkinson, , anti-Alzheimer, , analgesia, anticonvulsant activities, , and antitubercular treatments, suggesting a wide spectrum of therapeutic possibilities.…”

Section: Introductionmentioning

confidence: 99%

Evaluating the Neuroprotective Potential of Novel Benzodioxole Derivatives in Parkinson’s Disease via AMPA Receptor Modulation

Hawash,

Qneibi,

Natsheh

et al. 2024

ACS Chem. Neurosci.

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Parkinson’s disease (PD) is a significant health issue because it gradually damages the nervous system. α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors play a significant role in the development of PD. The current investigation employed hybrid benzodioxole-propanamide (BDZ-P) compounds to get information on AMPA receptors, analyze their biochemical and biophysical properties, and assess their neuroprotective effects. Examining the biophysical characteristics of all the subunits of the AMPA receptor offers insights into the impact of BDZ-P on the desensitization and deactivation rate. It demonstrates a partial improvement in the locomotor capacities in a mouse model of Parkinson’s disease. In addition, the in vivo experiment assessed the locomotor activity by utilizing the open-field test. Our findings demonstrated that BDZ-P7 stands out with its remarkable potency, inhibiting the GluA2 subunit nearly 8-fold with an IC50 of 3.03 μM, GluA1/2 by 7.5-fold with an IC50 of 3.14 μM, GluA2/3 by nearly 7-fold with an IC50 of 3.19 μM, and GluA1 by 6.5-fold with an IC50 of 3.2 μM, significantly impacting the desensitization and deactivation rate of the AMPA receptor. BDZ-P7 showed an in vivo impact of partially reinstating locomotor abilities in a mouse model of PD. The results above suggest that the BDZ-P7 compounds show great promise as top contenders for the development of novel neuroprotective therapies.

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“…The pharmacophore model for anticonvulsant drugs consists of four binding sites by way of illustration; an aryl hydrophobic binding site (A), a hydrogen bonding domain (HBD), an electron donor-acceptor system (D), and a hydrophobic aryl ring (C). 32 The standard drug phenytoin and phenobarbital are considered as references for designing the pharmacophore model of newly synthesized compounds ( Figure 1 ). 33 , 34 …”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis,In Vivo, andIn SilicoEvaluation of Benzothiazoles Bearing a 1,3,4-Oxadiazole Moiety as New Antiepileptic Agents

et al. 2023

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In the presented manuscript, a new series of 2-[4-methoxy-3-(5-substituted phenyl-[1,3,4]oxadiazol-2-ylmethoxy)-phenyl]-benzothiazoles ( 6a–n ) have been synthesized and studied in vivo and in silico for their anticonvulsant potential. Maximum electroshocks (MES) and subcutaneous pentylenetetrazol (scPTZ) models have been used for in vivo anticonvulsant activity. Auto Dock 4.2 software was used for in silico studies, and the targeted protein was 5IOV.sThe antidepressant activity of selected compounds (most active) was determined as a reduction in locomotor activity through an actophotometer. In vivo and In silico studies proved that among all the synthesized compounds, 6f, 6h, 6j, and 6l were the most potent with no neurotoxicity as compared to conventional drugs (phenytoin and phenobarbital). The in silico studies also indicated about different binding interactions of synthetic compounds to localize the binding receptors. The most likely mode of action for these drugs, according to the docking analysis of active compounds with various targets, is their binding to the VGCC and NMDA receptors.

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Amide as a Potential Pharmacophore for Drug Designing of Novel Anticonvulsant Compounds

Cited by 7 publications

References 41 publications

The untold story of starch as a catalyst for organic reactions

The untold story of starch as a catalyst for organic reactions

Evaluating the Neuroprotective Potential of Novel Benzodioxole Derivatives in Parkinson’s Disease via AMPA Receptor Modulation

Design, Synthesis,In Vivo, andIn SilicoEvaluation of Benzothiazoles Bearing a 1,3,4-Oxadiazole Moiety as New Antiepileptic Agents

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