Recent Advancement in Synthesis of Isatin as Anticonvulsant Agents: A Review

Nain, Sumitra

doi:10.4172/2161-0444.1000173

Cited by 15 publications

(6 citation statements)

References 106 publications

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“…After standing for 90 min, the final product was filtered with suction pump followed by washing with cold water to remove sulphuric acid and dried in air. 12,13…”

Section: Methodsmentioning

confidence: 99%

“…After standing for 90 min, the final product was filtered with suction pump followed by washing with cold water to remove sulphuric acid and dried in air. 12,13 Preparation of 1-(2'-amino substituted phenyl)-2-(piperidin-1-yl)ethane-1,2-dione. A solution (10 mL) of isatin derivatives 2a-g (2 mmol) and piperidine (4 mmol) in 80% aqueous MeOH was refluxed for 3 hours.…”

Section: Preparation Of Five and 7-substituted Isatinmentioning

confidence: 99%

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Entropy controlled reaction of piperidine with isatin derivatives in 80% aqueous methanol

El-Rahman,

Ibrahim,

Fathalla

et al. 2023

Progress in Reaction Kinetics and Mechanism

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The reactions of 5- and 7-substituted isatin derivatives (H, Me, Cl, Br) with piperidine in 80% aqueous methanol gave the corresponding 1-(2’-amino-5’- or 3’- substituted phenyl)-2-(piperidin-1-yl) ethane-1,2-dione derivatives. The reaction is proceeded through nucleophilic attack on C-2 followed by ring opening process. The reaction showed a second order and the isokinetic temperature is 169 K indicating that the reaction is entropy controlled. The constant ∆G# value, the linear plot of ∆H# versus ∆S#, plot of log kN values at high temperature versus those at low temperatures indicated that a unified mechanism of the reactions for all substituents. The σo-Taft's constants are linearly correlated with log kN values and the ρ values are (2.01–1.86) pointing out that inductive effect of substituent is predominant and the rate-limiting is the breakdown of the tetrahedral intermediate T− and the ring opening is catalyzed by water.

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“…After standing for 90 min, the final product was filtered with suction pump followed by washing with cold water to remove sulphuric acid and dried in air. 12,13…”

Section: Methodsmentioning

confidence: 99%

Section: Preparation Of Five and 7-substituted Isatinmentioning

confidence: 99%

Entropy controlled reaction of piperidine with isatin derivatives in 80% aqueous methanol

El-Rahman,

Ibrahim,

Fathalla

et al. 2023

Progress in Reaction Kinetics and Mechanism

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“…This method involves the characteristics relationship between electrons donating, an electron withdrawing group, to convert aniline to intermediate 3-methylthyiooxidinol. In this intermediate, the methyl group is oxidized by N-chlorosucinamide, which is proceeded by the hydrolysis of the chlorinated intermediate [25,26] (Figure 4).…”

Section: Gassman Synthesismentioning

confidence: 99%

Synthesis of Isatin and Its Derivatives and their Applications in Biological System

Aziz

Ullah²,

Ullah³

et al. 2020

BJSTR

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Here investigations were made to study the variant developments in the synthesis of isatin and its derivatives. This review comprehended the various synthetic methods especially, sandmeyer synthesis, stolle synthesis and gassman synthesis for the synthesis of isatin. The isatin and its derivatives played a key role in biomedical applications. The isatin and its derivatives are used as bactericide, fungicide, anti-HIV, anti-epileptic, anti-instigative and so on. The isatin derivatives are helpful in inhibiting the activity of the urease and α-glucosidase enzymes and reduce the risks of pyelonephritis, gastric problems and diabetes. This review highlighted the synthetic routes for the synthesis of isatin and the beneficial aspects of isatin and its derivatives in biomedical field.

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“…An indole backbone, with various substituents on the core structure, has the ability to display a spectrum of functionalities. In particular, and due to their broad structural diversity, isatins have been shown to affect a wide range of biological targets [35][36][37][38][39]. We computationally screened a variety of isatin derivatives against HAV 3C protease, and found that two modifications in the protecting groups of isatins (in compounds 8 and 9; Table 1) resulted in better interactions with the target, as reflected in docking studies as well as in the 100 ns molecular dynamics simulations.…”

Section: Novel Isatin-based Compounds Against Hav 3cmentioning

confidence: 99%

Toward development of generic inhibitors against the 3C proteases of picornaviruses

Banerjee¹,

Bhat

Rao

et al. 2018

The FEBS Journal

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Development of novel antivirals, which requires knowledge of the viral life cycle in molecular detail, is a daunting task, involving extensive investments, and frequently resulting in failure. As there exist significant commonalities among virus families in the manner of host interaction, identifying and targeting common rather than specific features may lead to the development of broadly useful antivirals. Here, we have targeted the 3C protease of Hepatitis A Virus (HAV), a feco‐orally transmitted virus of the family Picornaviridae, for identification of potential antivirals. The 3C protease is a viable drug target as it is required by HAV, as well as by other picornaviruses, for post‐translational proteolysis of viral polyproteins and for inhibiting host innate immune pathways. Computational screening, followed by chemical synthesis and experimental validation resulted in identification of a few compounds which, at low micromolar concentrations, could inhibit HAV 3C activity. These compounds were further tested experimentally against the 3C protease of Human Rhinovirus, another member of the Picornaviridae family, with comparable results. Computational studies on 3C proteases from other members of the picornavirus family have indicated that the compounds identified could potentially be generic inhibitors for picornavirus 3C proteases.

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Recent Advancement in Synthesis of Isatin as Anticonvulsant Agents: A Review

Cited by 15 publications

References 106 publications

Entropy controlled reaction of piperidine with isatin derivatives in 80% aqueous methanol

Entropy controlled reaction of piperidine with isatin derivatives in 80% aqueous methanol

Synthesis of Isatin and Its Derivatives and their Applications in Biological System

Toward development of generic inhibitors against the 3C proteases of picornaviruses

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