ChemInform Abstract: Some 3‐Hydrazono‐2‐indolinones and N‐Mannich Bases as Potential Anticonvulsants.

Guersoy, A.; Karalı, Nilgün; Bueyuektimkin, S.; Demirayak, Şeref; Ekinci, A. C.; Oezer, H.

doi:10.1002/chin.199645144

Cited by 6 publications

(6 citation statements)

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“…The anticonvulsant activity of derivates of indole‐based hydrazones with indole‐3‐carboxaldehyde hydrazones ( 33 and 34 ) were studied in the MES test [Popp, ]. A series of 3‐aryloxy/arylthioxyacetyl hydrazono‐2‐indolinones synthesized by condensation of isatin with aryloxy/arythioxyacetylhydrazines and treatment with morpholine and formaldehyde resulted in the 1‐morpholinomethyl‐3‐aryloxy/arylthioxyacetylhydrazono‐2‐indolinones ( 35 and 36 ) [Gürsoy et al, ] that exhibited different anticonvulsant activity in scPTZ test.…”

Section: Pharmacologial Screening Of Hydrazide/hydrazone Derivatives mentioning

confidence: 99%

Recent Developments of Hydrazide/Hydrazone Derivatives and Their Analogs as Anticonvulsant Agents in Animal Models

Angelova

Karabeliov

Andreeva-Gateva

et al. 2016

Drug Development Research

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Preclinical Research Epilepsy is a chronic devastating neurological disorder characterized by synchronous interictal discharges. Treatment with antiepileptic drugs (AEDs) can alleviate spontaneous seizure activity without preventing the progression and development of epileptogenesis. Current design and development of new AEDs and strategies for the prevention of epilepsy is focused mainly on attenuating uncontrolled seizures, severe side effects and toxicity in chronic drug therapy. It has thus become necessary to discover new chemical pharmacophores with a broad spectrum of activity and less neurotoxicity. Hydrazide/hydrazone derivatives that possess a -CO-NHN=CH- group constitute an important class of compounds for drug development. This review highlights the specific characteristics of various hydrazide/hydrazone derivatives and structurally related semicarbazones, semicarbazides and Schiff base compounds and their anticonvulsant activities. It is focused on the influence of differently substituted pharmacophores developed through SAR studies and testing their activity against different pharmcological targets. Drug Dev Res 77 : 379-392, 2016. © 2016 Wiley Periodicals, Inc.

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Section: Pharmacologial Screening Of Hydrazide/hydrazone Derivatives mentioning

confidence: 99%

Recent Developments of Hydrazide/Hydrazone Derivatives and Their Analogs as Anticonvulsant Agents in Animal Models

Angelova

Karabeliov

Andreeva-Gateva

et al. 2016

Drug Development Research

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“…8, 9 Mannich bases of isatin and their derivatives were synthesized and reported for antibacterial, 10 antifungal, 11 anti-HIV, [12][13][14][15][16][17][18][19] anticonvulsant activities 20 and GAL3 receptor antagonist activity 21,22 and in recent years the compounds showing potent cytotoxicity in vitro 9 and antiviral activity 23 have been reported, among others ( Figure 2). In continuation of our work on bioactive isatin, 24 encouraged by the observations about biological properties of isatin derivatives and 1,4-benzothiazine, we decided to design and synthesize Mannich bases containing both 1,4-benzothiazine and isatin moieties to generate a series of newer 1,4-benzothiazine derivatives and screen them for potential biological activity.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of 1,4‐Benzothiazine Compounds Containing Isatin Hydrazone Moiety as Antimicrobial Agent

et al. 2009

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A series of novel 3-methyl-N"-(2-oxoindolin-3-ylidene)-4H-benzo [b][1,4]thiazine-2-carbohyrazides have been synthesized and studied on their in vitro antimicrobial activity potency to establish structure-activity relationship. Several compounds demonstrated promising antifungal and antibacterial activity; however, other tested compounds exhibited moderate to poor antimicrobial activity with respect to the reference drug against the test strains.

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“…primary amine or ammonia) [16]. These compounds have several biological activities such as antimicrobial [5-91, cytotoxic [10-15], anticancer [16], analgesic and anti-inflammatory [17][18][19], and anticonvulsant activity [20][21][22][23]. Having the anticonvulsant activity of Mannich bases of conjugated arylidene ketones [22], Mannich bases of 1-aryl-l-ethanones [24], 3,3'-methylimino bis(l-aryl-l-propanone)hydrochlorides, which are bisMannich bases derived from acetophenone and 1-methyl-3-aroyl-4-phenyl-4-piperidinol hydrochlorides [21] led us to design and synthesize some mono-Mannich bases, 3-amino-l-aryl-l-propanone hydrochlorides (Ig1-Ig4), to investigate their anticonvulsant activities.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Some Mono-Mannich Bases and Corresponding Azine Derivatives and Evaluation of their Anticonvulsant Activity

Gül

Calis

Vepsäläinen

2011

Arzneimittelforschung

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Mono-Mannich bases, 3-amino-1-aryl-1-propanone hydrochlorides (Ig1-Ig4), and their corresponding azine derivatives, N,N'-bis(3- amino-1-aryl-propylidene) hydrazine dihydrochlorides (D1-D4), were synthesized and their anticonvulsant activities were evaluated. Alterations in biological activity depending on modifications in chemical structure were also followed. The aryl part was phenyl in Ig1, D1, Ig2, D2, Ig3, D3, or p-hydroxyphenyl in Ig4, and D4. The amine part was dimethylamine in Ig1, D1, Ig4, and D4, piperidine in Ig2, D2 or morpholine in Ig3, D3. Compounds D2, D3, and D4 are new. The anticonvulsant activity was determined by maximal electroshock (MES) and subcutaneous metrazole (pentetrazol; scMet) tests. The rotorod toxicity test was used for determining neurological deficits. While the compounds were not effective in scMet, they were found to exert protective effect in MES. The results of MES are as follows: Compound [dose level (mg/kg), time (h)]: Ig1 [30 (0.5 h), 100 (0.5 h)]; Ig2 [30 (0.5 h, 4 h)]; Ig3 [30 (0.5 h), 100 (0.5 h), 300 (0.5 h, 4 h)]; Ig4 [300 (0.5 h, 4 h), 100 (4 h)]; D1 [30 (0.5 h)]; D3 [100 (0.5 h,4 h), 300 (0.5 h), 30 (4 h)]]; D4 [300 (0.5 h, 4 h)]. D2 did not show any anticonvulsant activity in both tests. Ig1, Ig2, D1, D2, and D3 exhibited neurotoxicity. Compounds Ig2, D1, and D2 were neurotoxic at 100 mg/kg dose level at 0.5 h. Ig1 was neurotoxic at 300 mg at 0.5 h, D3 was neurotoxic at 300 mg at 4 h. Conversion of mono-Mannich bases to their corresponding azine derivatives generally decreased the anticonvulsant activity. Ig3, Ig4 and D4 seem to be promising candidates to develop new anticonvulsant compounds for grand mal epilepsy for further synthesis and in vivo studies, since they were effective in MES screening and no neurotoxicity was observed with them.

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ChemInform Abstract: Some 3‐Hydrazono‐2‐indolinones and N‐Mannich Bases as Potential Anticonvulsants.

Cited by 6 publications

References 0 publications

Recent Developments of Hydrazide/Hydrazone Derivatives and Their Analogs as Anticonvulsant Agents in Animal Models

Recent Developments of Hydrazide/Hydrazone Derivatives and Their Analogs as Anticonvulsant Agents in Animal Models

Synthesis of 1,4‐Benzothiazine Compounds Containing Isatin Hydrazone Moiety as Antimicrobial Agent

Synthesis of Some Mono-Mannich Bases and Corresponding Azine Derivatives and Evaluation of their Anticonvulsant Activity

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