scholarly journals Anticonvulsant Activities of 4-benzylidene-6-(4-methyl-phenyl)-4,5-dihydropyridazin-(2H)-ones and 4-benzylidene-6-(4-chloro-phenyl)-4,5-dihydropyridazin-(2H)-ones

2016 ◽  
Vol 3 (1) ◽  
pp. 203-214 ◽  
Author(s):  
Mohammad Asif ◽  
Anita Singh
Keyword(s):  
Maximum Activity ◽  
Anticonvulsant Agents ◽  
Phenytoin Sodium ◽  
Methyl Derivatives ◽  
Chloro Derivatives ◽  
Anticonvulsant Activities ◽  
Dose Levels ◽  
Near Future ◽  
Methyl Phenyl

Background: Two series of 4-benzylidene-6-(4-methyl-phenyl)-4,5-dihydropyridazin-(2H)-one compounds (3a-e) and 4-benzylidene-6-(4-chloro-phenyl)-4,5-dihydropyridazin-(2H)-ones (3f-j) were synthesized and evaluated as anticonvulsant agents. Methods: Synthesized compounds (3a-3j) were tested against maximum electro shock (MES) and Isoniazid (INH) induced convulsion methods for anticonvulsant activities and neurotoxicity. Results: In MES induced convulsions, result found that the compounds 3e and 3j exhibited highest anticonvulsant activities. In INH induced convulsions, result was indicated that all the compounds exhibited good anticonvulsant activities., whereas compounds 3d and 3j showed maximum activity. Methyl derivatives were more active than chloro derivatives. Phenytoin sodium (25mg/kg) and sodium vaproate (50mg/kg) were used as reference drugs. All these synthesized pyridazinone compounds (3a-j) did not exhibit any neurotoxicity up to 100 mg/kg dose levels. Conclusion: All compounds showed good anticonvulsant activities against both MES and INH induced convulsion models. Many such explorations are anticipated in the near future.

Geoeffective events through solar cycles

2018 ◽  
Vol 13 (S340) ◽  
pp. 255-256
Author(s):  
Brigitte Schmieder ◽  
Guillaume Aulanier
Keyword(s):  
Field Strength ◽  
Maximum Activity ◽  
Solar Cycles ◽  
Geomagnetic Disturbances ◽  
Historical Databases ◽  
Solar Events ◽  
Solar Storms ◽  
Near Future ◽  
Modern Era

AbstractExtreme solar storms are well known in the historical databases. Since the modern era, it has been possible to associate clearly geomagnetic disturbances with solar events (flares, SEP, CMEs). In the recent solar cycles the geoeffective events (number and strength) are decreasing. As an example, in the 2002 maximum activity year, we present how many flares, and CMEs were geoeffective. Based on observations and simulations, we discuss on the size of sunspots and the field strength to get more energetic flares (> 1032 ergs) in the near future.

SYNTHESIS AND EVALUATION OF SOME NEWER QUINAZOLINONYL SUBSTITUTED BENZOXAZEPINYL / BENZOTHIAZEPINYL INDOLES AS POTENT ANTICONVULSANT AGENTS

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (03) ◽  
pp. 18-24
Author(s):  
Archana ◽  
Keyword(s):  
Nmr Spectroscopy ◽  
Acute Toxicity ◽  
1H Nmr ◽  
Elemental Analysis ◽  
Anticonvulsant Activity ◽  
1H Nmr Spectroscopy ◽  
Standard Drug ◽  
Anticonvulsant Agents ◽  
Phenytoin Sodium

new series of 3-[3-amino-2-methyl-6-substituted quinazolin-4(3H)-onyl chalconyl)-2-substituted indoles (3-8), 3-[3-Amino-2-methyl-6- substituted quinazolin-4(3H) -onyl-benzoxazepin/benzo -thiazepin- 2-yl] -2-substituted indoles (9-20) and 3-[3-amino-2-methyl-6-substituted quinazolin-4(3H) -onyl-3- (sub-stituted phenylaminomethylene) -benzoxazepin/benzothizepin-2-yl] -2-substitutedindoles (21-44) were synthesised and evaluated for anticonvulsant activity. All these compounds were screened in vivo, for their anticonvulsant activity and acute toxicity. Coumpund 44 , 3-[3-amino-2-methyl-6-bromoquinazolin- 4(3H)-onyl-3- (chlorophenylaminomethylene)-benzothiazepine-2-yl]-2-chloroindole, was found to be most potent compound of this series , more potent than standard drug phenytoin sodium. The homogeneity of all the compounds have been established by elemental analysis, IR and 1H-NMR spectroscopy.

Synthesis and Pharmacological Evaluation of New Indolyl-oxadiazoles as Anticonvulsant Agents

2009 ◽  
Vol 2 (3) ◽  
pp. 661-666
Author(s):  
Harish Rajak ◽  
Ravichandran Veerasamy ◽  
Arun Kumar Gupta ◽  
Murli Dhar Kharya ◽  
Pradeep Mishra
Keyword(s):  
1H Nmr ◽  
13C Nmr ◽  
Anticonvulsant Activity ◽  
Anticonvulsant Drug ◽  
Maximal Electroshock ◽  
Maximal Electroshock Seizure ◽  
Anticonvulsant Agents ◽  
Pharmacological Evaluation ◽  
Anticonvulsant Activities

The search for better anticonvulsant drug and the importance of 2,5-disubstituted 1,3,4-oxadiazoles and indole as anticonvulsant pharmacophores, prompted us to design, synthesize and evaluate a series of differently substituted 1,3,4-oxadiazoles for their potential anticonvulsant activity. The structures of the compounds were elucidated by elemental and spectral (IR, 1H NMR, 13C NMR and MS) analyses. Most of the test compounds demonstrated appreciable anticonvulsant activities in maximal electroshock seizure (MES) and subcutaneous pentylenetrtrazole (scPTZ) models.

scholarly journals DESIGN, FACILE SYNTHESIS, AND BIOLOGICAL EVALUATION OF NOVEL 1,3-THIAZINE DERIVATIVES AS POTENTIAL ANTICONVULSANT AGENTS

2016 ◽  
Vol 9 (5) ◽  
pp. 272 ◽  
Author(s):  
Ravindar B ◽  
Srinivasa Murthy M ◽  
Afzal Basha Shaik
Keyword(s):  
Small Molecules ◽  
Anticonvulsant Activity ◽  
Aromatic Aldehydes ◽  
Biological Evaluation ◽  
Important Class ◽  
Facile Synthesis ◽  
Anticonvulsant Agents ◽  
Anticonvulsant Activities ◽  
Synthesis And Biological Evaluation

ABSTRACTObjective: Chalcones and their heterocyclic analogs represent an important class of small molecules having anticonvulsant activities. Therefore, inthis study, the synthesis and anticonvulsant activity of some new chalcones and 1,3-thiazines were described.Methods: The reaction of 1-acetylnaphthalene with substituted aromatic aldehydes in the presence of aq. NaOH afforded corresponding chalconeswhich upon further cyclization with thiourea resulted in 1,3-thiazine derivatives. The newly synthesized compounds were tested for anticonvulsantactivity by pentylenetetrazole-induced seizures method using diazepam as standard.Results: Most of the compounds showed good anticonvulsant activity but is less than diazepam. 1,3-thiazines were more potent than chalconesand among them, compound P4 containing 4-fluorophenyl substituents on the thiazine moiety was more potent as it has prolonged the onset ofconvulsions by 155.2 seconds.Conclusion: We described the synthesis and anticonvulsant activity of novel chalcones and 1,3-thiazine derivatives. 1,3-thiazines are more activeanticonvulsant agents than chalcones and in particular compounds with electron withdrawing substituents.Keywords: Chalcone, 1,3-thiazine, Pentylenetetrazole.

Analgesic and Anticonvulsant Activities of Some Newly Synthesized Trisubstituted Pyridine Derivatives

2013 ◽  
Vol 68 (7-8) ◽  
pp. 264-268 ◽  
Author(s):  
Osama I. Abdel Salam ◽  
Mohamed A. Al-Omar ◽  
Nagy M. Khalifa ◽  
Abd El-Galil E. Amr ◽  
Mohamed M. Abdallah
Keyword(s):  
Isonicotinic Acid ◽  
Acid Hydrazide ◽  
Isonicotinic Acid Hydrazide ◽  
Pyridine Derivatives ◽  
Anticonvulsant Agents ◽  
Pharmacological Screening ◽  
Anticonvulsant Activities

A series of novel pyridine carbohydrazide derivatives were synthesized from the reaction of 2-chloro-6-hydrazino-isonicotinic acid hydrazide with selected active reagents. All prepared compounds were tested as analgesic and anticonvulsant agents. The pharmacological screening showed that many of these compounds have good activities comparable to those of valdecoxib and carbamazepine as reference drugs

Spectrophotometric reductions with an IBM 1620

1966 ◽  
Vol 24 ◽  
pp. 116-117
Author(s):  
P.-I. Eriksson
Keyword(s):  
Astronomical Data ◽  
Spectrophotometric Data ◽  
Electronic Computers ◽  
The University ◽  
Near Future

Nowadays more and more of the reductions of astronomical data are made with electronic computers. As we in Uppsala have an IBM 1620 at the University, we have taken it to our help with reductions of spectrophotometric data. Here I will briefly explain how we use it now and how we want to use it in the near future.

Recent developments in automated Transmission Electron MI

1989 ◽  
Vol 47 ◽  
pp. 46-47
Author(s):  
W.J. de Ruijter ◽  
P. Rez ◽  
David J. Smith
Keyword(s):  
Image Analysis ◽  
Computer Image ◽  
Lens Design ◽  
Computer Image Analysis ◽  
Transmission Electron ◽  
Resolution Electron ◽  
Recent Developments ◽  
On Line ◽  
Routine Procedures ◽  
Near Future

There is growing interest in the on-line use of computers in high-resolution electron n which should reduce the demands on highly skilled operators and thereby extend the r of the technique. An on-line computer could obviously perform routine procedures hand, or else facilitate automation of various restoration, reconstruction and enhan These techniques are slow and cumbersome at present because of the need for cai micrographs and off-line processing. In low resolution microscopy (most biologic; primary incentive for automation and computer image analysis is to create a instrument, with standard programmed procedures. In HREM (materials researc computer image analysis should lead to better utilization of the microscope. Instru (improved lens design and higher accelerating voltages) have improved the interpretab the level of atomic dimensions (approximately 1.6 Å) and instrumental resolutior should become feasible in the near future.

Intraneuronal accumulations of lysosomes in the cerebellum of rats and dogs after dosing with MDL-832

1990 ◽  
Vol 48 (3) ◽  
pp. 830-831
Author(s):  
S.D. Barnard ◽  
S.D. Warner
Keyword(s):  
Brown Pigment ◽  
Beagle Dogs ◽  
Sprague Dawley ◽  
Gelatin Capsules ◽  
Pigment Granules ◽  
Sprague Dawley Rats ◽  
Hematoxylin And Eosin ◽  
Dose Levels

1, 2, 9, 10-tetramethoxyaporphine phosphate (MDL-832) was once considered a potential human antitussive. MDL-832 was administered orally in the diets of Sprague-Dawley rats at dose levels of 0, 5, 10, 20, 40, 80 and 160 mg/kg/day for 3 and 6 months and in gelatin capsules to Beagle dogs at 0, 5, 10, 15, 30 and 60 mg/kg/day for 3, 6 and 12 months. Histopathologic examinations of hematoxylin and eosin-stained cerebellar sections revealed intracytoplasmic brown pigment accumulations in large fusiform neurons (presumably the motor type) of the pons. The pigment granules were found to be PAS-positive, non-acid fast, iron-free, Sudan B-positive and fuchsinophilic. Intraneuronal pigment accumulations were seen in rats after 3 months of treatment at 80 mg but not at 40 mg and after 6 months at 20 mg but not at 10 mg. For dogs the effect was observed after 3 months at 60 mg but not at 30 mg and after 12 months at 10 mg but not at 5 mg.

DNA methylation in satellite repeats disorders

2019 ◽  
Vol 63 (6) ◽  
pp. 757-771 ◽  
Author(s):  
Claire Francastel ◽  
Frédérique Magdinier
Keyword(s):  
Dna Methylation ◽  
Human Genome ◽  
Repetitive Dna ◽  
Dna Sequences ◽  
Satellite Repeats ◽  
Tremendous Progress ◽  
Genes Encoding ◽  
Dna Elements ◽  
Near Future

Abstract Despite the tremendous progress made in recent years in assembling the human genome, tandemly repeated DNA elements remain poorly characterized. These sequences account for the vast majority of methylated sites in the human genome and their methylated state is necessary for this repetitive DNA to function properly and to maintain genome integrity. Furthermore, recent advances highlight the emerging role of these sequences in regulating the functions of the human genome and its variability during evolution, among individuals, or in disease susceptibility. In addition, a number of inherited rare diseases are directly linked to the alteration of some of these repetitive DNA sequences, either through changes in the organization or size of the tandem repeat arrays or through mutations in genes encoding chromatin modifiers involved in the epigenetic regulation of these elements. Although largely overlooked so far in the functional annotation of the human genome, satellite elements play key roles in its architectural and topological organization. This includes functions as boundary elements delimitating functional domains or assembly of repressive nuclear compartments, with local or distal impact on gene expression. Thus, the consideration of satellite repeats organization and their associated epigenetic landmarks, including DNA methylation (DNAme), will become unavoidable in the near future to fully decipher human phenotypes and associated diseases.

Sign in / Sign up

Export Citation Format

Share Document