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Query: UMLS:C0036572 (seizures)
 80,221 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

A series of alkanolamides and alkanoamines derivatives of xanthone were prepared and evaluated for antiepileptic activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazol seizure threshold (ScMet) assays and for neurotoxicity (TOX). Several analogues from the appropriate alkanolamines were found to be active in both the anticonvulsant tests. Most interesting were the anticonvulsant results of the appropriate 2-amino- or 2-N-methylamino-1-butanol derivatives of 7-chloroxanthone 8-11, which displayed anti-MES activity with a protective index (TD50/ED50) in the range 2.84-3.62 for 8-11 corresponding with that for phenytoin, carbamazepine and valproate.
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PMID:Evaluation of some 2-substituted derivatives of xanthone for anticonvulsant properties. 967 71

Synthesis and physicochemical properties of alkanolamine derivatives of xanthone are described. Alkanolamines were synthesized by of the reaction of an appropriate aminoalcohol with corresponding 2-bromomethylxanthones. The obtained compounds 1-13 were evaluated for anticonvulsant activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole seizure threshold (scMet) assays and for neurotoxicity (TOX). Several alkanolamines were found to be active in both the anticonvulsant tests. Most interesting were the 2-amino-1-propanol-, 1-amino-2-propanol- or 1-amino-2-butanol derivatives of 6-methoxy- or 6-chloroxanthone, which displayed anti MES activity with a protective index (TD50/ED50) in the range 2.21-5.84 corresponding with that for phenytoin, carbamazepine and valproate.
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PMID:Synthesis and anticonvulsant effects of some aminoalkanolic derivatives of xanthone. 981 32

A series of 1,2-aminoalkanol derivatives were prepared and evaluated for anticonvulsant activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole seizure threshold (scMet) assays and for neurotoxicity (TOX). Most interesting were the anticonvulsant results of S-(+)-2-amino-1-butanol derivative VIII, which displayed anti-MES activity with a protective index (TD50/ED50) of 4.55 corresponding with that for phenytoin, carbamazepine and valproate.
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PMID:Synthesis and anticonvulsant activity of 1,2-aminoalkanol derivatives. 1007 36

A series of appropriate aminoisopropanoloxy derivatives of 2-, 3- or 6-xanthone was synthesized and evaluated for anticonvulsant activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole seizure threshold (ScMet) assays and for neurotoxicity (TOX). The most interesting result was the anticonvulsant activity of (+/-)-3-(2-propylamino)-1- [(2-methyl)-6-xanthonoxy]-2-propanol hydrochloride (10), which displayed anti-MES activity with a protective index (TD50/ED50) of 0.80. Some of the obtained compounds were also tested for their effect on the circulatory system (influence on the non-working heart perfusion, protection against adrenaline induced-arrhythmia) and acute toxicity.
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PMID:Pharmacological properties of some aminoalkanolic derivatives of xanthone. 1148 77

A series of alkanolamides have been tested for anticonvulsant activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole seizure treshold (ScMet) assays and for neurotoxicity (TOX) in rodents. Most interesting were the anticonvulsant results of 2N-methylaminoethanol derivative II, which displayed anti-MES activity (mice) with a protective index (TD50/ED50) of 2.536 higher than that for valproate.
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PMID:Preliminary evaluation of anticonvulsant activity of some 4-(benzyloxy)-benzamides. 1508 May 96

A series of appropriate aminoalkanolic derivatives 2- or 4-methylxanthone was synthesized and evaluated for anticonvulsant activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole seizure threshold (scPtz) assays, and for neurotoxicity (TOX). The most interesting result was the anticonvulsant activity of (R,S)-2N-(6-chloro-2-xanthonemethyl-2N-methylamino-1-propanol hydrochloride (II, which displayed anti-MES and anti-scPtz activity. Some of the obtained compounds (I - IV and V - VII) were also tested for their effect on the circulatory system (the effect on normal electrocardiogram, protection against adrenaline-, barium-, calcium- and/or strophanthine-induced arrhythmias, the effect on the arterial blood pressure and respiratory movements) and acute toxicity.
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PMID:The influence of some aminoalkanolic xanthone derivatives on central nervous and cardiovascular systems in rodents. 1588 6

Various 1,4-substituted derivatives of piperazine (I-XII) were synthesized and evaluated for their anticonvulsant activity in the maximal electroshock (MES) and subcutaneous pentylenetetrazole (ScMet)--induced seizures and for neurotoxicity (TOX) in the rotorod test in mice and rats. The most promising compounds seem to be 1-[(2,4,6-trimethyl)-phenoxyethyl]-4-(2-hydroxyethyl)-piperazine dihydrochloride (II) and 1,4-bis-[(4-chloro-3-methyl)-phenoxyethyl]-piperazine dihydrochloride (X) which displayed anti-MES activity with their protective index (PI) higher than that for valproate II (rats), X(mice)).
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PMID:Synthesis and anticonvulsant activity of some piperazine derivatives. 1588 10

To continue our systematic SAR studies, two series of N-benzyl- (X=CH2) and N-aminophenyl- (X=NH) derivatives of 2-azaspiro[4.4]nonane (1a-1j) and 2-azaspiro[4.5]decane-1,3-dione (2a-2j) were synthesized, and evaluated in maximum electroshock seizure (MES), subcutaneous pentylenetetrazole (sc.MET) and rotorod (TOX) tests for their anticonvulsant activity. Among those derivatives, the most potent N-aminophenyl-2-azaspiro[4.4]nonane-1,3-dione 1j had ED50=76.27 mg kg-1. X-ray structures for two pairs of derivatives with a different linker were solved. Then 3-D data for the active 1j versus less active 2j, both having an imine linker (X=NH), and the respective parent of compounds with a methylene linker (X=CH2) (1a and 2a) were discussed.
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PMID:Synthesis, physicochemical and anticonvulsant properties of N-benzyl and N-aminophenyl derivatives of 2-azaspiro[4.4]nonane and [4.5]decane-1,3-dione. Part I. 1595 Sep 73

A series of aroxyacetamides and aroxyethylamines were prepared and evaluated for anticonvulsant activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole seizure threshold (ScMet) assays and for neurotoxicity (TOX). Most of them exhibited anticonvulsant activity in the MES screen (mice, i.p.) in the doses up to 300 mg/kg b.w. The most active compound was XVI, which given in the dose 100 mg/kg b.w. produced 100% anticonvulsant protection after 0.5 h without neurotoxicity. The most promising compound in the VIa phase (rats, p.o.) was VIII, which produced higher anticonvulsant protection (to 75% at 0.5 h).
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PMID:Preliminary evaluation of anticonvulsant activity of some aroxyacetamides and aroxyethylamines. 1645 83

A series of appropriate alkanolamine and amide derivatives of xanthone were prepared and evaluated for anticonvulsant activity using maximal electroshock (MES) and subcutaneous pentylenetetrazole (scMet) induced seizures, and for neurotoxicity (TOX) using the rotorod test on mice and rats. The most promising compounds seem to be the appropriate aminoalkanolic derivatives of 6-chloroxanthone, among which the R-(-) and S-(+)-2amino-1-propanol derivatives of 6-chloro-2-methylxanthone (2(a) and 2(b)) displayed anti-MES activity (in mice) with a protective index (TD(50)/ED(50)) of 6.23<6.85, corresponding to that of phenytoin, carbamazepine and valproate. The most active compound, 2(b), was determined to have an affinity to the benzodiazepine (BDZ) receptor and voltage-dependent Ca(2+) channel (VDCC) by using radioligand binding assays. The enantiomeric purities of 2(a) and 2(b) were determined using an analytical liquid chromatography-mass spectrometry method.
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PMID:Anticonvulsant activity of some xanthone derivatives. 1864 Aug 43


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