Anticonvulsant evaluation of aminoalkanol derivatives of 2- and 4-methylxanthone.

@article{Szkaradek2013AnticonvulsantEO,
  title={Anticonvulsant evaluation of aminoalkanol derivatives of 2- and 4-methylxanthone.},
  author={Natalia Szkaradek and Agnieszka Gunia and Anna M Waszkielewicz and Lucyna Antkiewicz-Michaluk and Marek T. Cegła and Edward Szneler and Henryk Marona},
  journal={Bioorganic \& medicinal chemistry},
  year={2013},
  volume={21 5},
  pages={
          1190-8
        }
}
A series of 17 new aminoalkanol derivatives of 6-methoxy- or 7-chloro-2-methylxanthone as well as 6-methoxy-4-methylxanthone was synthesized and evaluated for anticonvulsant activity. All compounds were verified in mice after intraperitoneal (ip) administration in maximal electroshock (MES) and subcutaneous pentetrazole (scMet) induced seizures as well as neurotoxicity assessment. Eleven of the tested substances showed protection against electrically evoked seizures in the majority of the… Expand
Design, synthesis, and anticonvulsant activity of some derivatives of xanthone with aminoalkanol moieties
A series of new xanthone derivatives have been synthesized and evaluated for their anticonvulsant properties in the maximal electroshock, subcutaneous metrazole tests and for neurotoxicity in theExpand
Synthesis and evaluation of pharmacological properties of some new xanthone derivatives with piperazine moiety.
TLDR
Combining of xanthone with piperazine moiety resulted in obtaining of compounds with increased bioavailability after oral administration, and 6-methoxy-2-{[4-(benzyl)piperazin-1-yl]methyl}-9H-xanthen-9-one (5) proved best properties. Expand
Design, synthesis and cardiovascular evaluation of some aminoisopropanoloxy derivatives of xanthone.
TLDR
The results of this study suggest that new compounds with multidirectional activity in cardiovascular system might be found in the group of xanthone derivatives. Expand
Design, synthesis and evaluation of activity and pharmacokinetic profile of new derivatives of xanthone and piperazine in the central nervous system.
TLDR
The pharmacokinetic analysis of active compounds done by a non-compartmental approach have shown a rapid absorption of all studied molecules from intraperitoneal cavity and good penetration the blood-brain barrier after i.p. administration with brain to plasma ratios. Expand
Antiarrhythmic activity of some xanthone derivatives with β1-adrenoceptor affinities in rats.
TLDR
The results of this study suggest that new compounds with antiarrhythmic activity might be found in the group of xanthone derivatives, however weaker than that of propranolol. Expand
Preliminary assessment of mutagenic and anti-mutagenic potential of some aminoalkanolic derivatives of xanthone by use of the Vibrio harveyi assay.
TLDR
It is demonstrated that four bioactive derivatives of xanthone display no mutagenic activity in the V. harveyi assay, and compounds III and IV demonstrated considerable anti-mutagenic activities in this test. Expand
In Vivo Screening of Xanthones from Garcinia oligantha Identified Oliganthin H as a Novel Natural Inhibitor of Convulsions.
TLDR
The findings present the anticonvulsant activity of oliganthin H, provide a novel scaffold for further modifications, and highlight the xanthone skeleton as an attractive and reliable resource for the development of emerging AEDs. Expand
Novel approaches to anticonvulsant drug discovery
TLDR
It is likely that models of mimic chronic epilepsy will help bridge the gaps and aid in the discovery of novel antiepileptic drugs – ones that can effectively modify the course of the disease. Expand
Contribution of reactive oxygen species to the anticancer activity of aminoalkanol derivatives of xanthone
TLDR
It is demonstrated that novel aminoalkanol xanthones mediated their anticancer activity primarily through ROS elevation and enhanced oxidative stress, which led to mitochondrial cell death stimulation; this mechanism was similar to the activity of gambogic acid. Expand
Recent insight into the biological activities of synthetic xanthone derivatives.
  • Shagufta, I. Ahmad
  • Chemistry, Medicine
  • European journal of medicinal chemistry
  • 2016
TLDR
This review has compiled and discussed recent developments on the pharmacological profile of synthetic xanthone derivatives for different therapeutic targets and offers support in the development of new xanthones derivatives as therapeutic agents. Expand
...
1
2
...

References

SHOWING 1-10 OF 20 REFERENCES
Anticonvulsant activity of some xanthone derivatives.
A series of appropriate alkanolamine and amide derivatives of xanthone were prepared and evaluated for anticonvulsant activity using maximal electroshock (MES) and subcutaneous pentylenetetrazoleExpand
Xanthone analogues of clofibrate / Synthesis and biological evaluation as antagonists of lipolysis in vitro.
TLDR
By appropriate superimposing of fenofibrate and fen ofibric acid molecules, two xanthone derivatives (closed models) may be obtained and very promising for further studies is the chlorine-free 3-isomer (3e). Expand
(2-Arylhydrazonomethyl)-substituted xanthones as antimycotics: synthesis and fungistatic activity against Candida species.
A series of arylhydrazones derived from various 6,8-diacetoxy- or 6,8-dihydroxy-9-oxo-9H-xanthene carboxaldehydes were synthesized and evaluated for their in vitro antifungal properties against twoExpand
Preclinical Development of Antiepileptic Drugs: Past, Present, and Future Directions
TLDR
The present review describes the current approach used in the search for new AEDs and offers some insight into future directions incorporating new and emerging models of therapy resistance and epileptogenesis. Expand
Comparative assay of an antiepileptic drugs by psychomotor seizure test and minimal electroshock threshold test.
TLDR
It is more difficult to prevent experimental "psychomotor" seizures with drugs than to elevate the threshold for minimal electroshock seizures, and drugs ineffective in psychomotor epilepsy rank higher than does Phenurone, an agent acknowledged to be superior in the management of this disorder. Expand
Potential antitumor agents. 58. Synthesis and structure-activity relationships of substituted xanthenone-4-acetic acids active against the colon 38 tumor in vivo.
TLDR
5-Methylxanthenone-4-acetic acids has a similar level of activity to that of flavoneacetic acid in the test systems employed but is more than 7-fold as dose potent, with 5-substituted compounds being clearly the most dose potent. Expand
Development of new antiepileptic drugs: challenges, incentives, and recent advances
Despite the introduction of many second-generation antiepileptic drugs (AEDs) in the past 15 years, a third of patients with epilepsy remain refractory to available treatments, and newer and moreExpand
Preliminary evaluation of pharmacological properties of some xanthone derivatives.
TLDR
The data obtained via receptor binding assay are in agreement with pharmacological results and could explain antiarrhythmic and/or hypotensive activity of the newly synthesized structures. Expand
Studies on uricosuric diuretics. I. Syntheses and activities of xanthonyloxyacetic acids and dihydrofuroxanthone-2-carboxylic acids.
TLDR
A series of substituted xanthonyloxyacetic acids (5 and 6), 1,2-dihydrofuro[2,3-c]xanthone-2-carboxylic acids (7) and 2,3.xanthon-3-yloxyacetics acids (8) showed potent diuretic activities, while 8 had lower activities. Expand
Antifungal and Antibacterial Activity of the Newly Synthesized 2‐Xanthone Derivatives
TLDR
A series of 2‐substituted xanthone derivatives 8–20 containing selected allyl, cinnamyl, morpholine, and imidazole moieties were synthesized and tested for their antifungal and antibacterial in‐vitro properties, showing significant efficacy against evaluated yeasts and dermatophytes. Expand
...
1
2
...