Biological anticonvulsant activity

No natural products or their analogues are included among the pyridopyridazines, but several interesting biologically active compounds have emerged. Some l-chloro-4-hydrazino- and 4-chloro-l-hydrazino-pyrido[2,3-d]pyridazines (460) are very active hypotensives, whilst related dialkoxy compounds have anticonvulsant activity (65CPB586). 

T. Murakami, E. Shek, E. Pop, N. Bodor, Improved Anticonvulsant Activity of Pheny-toin by a Redox Brain Delivery System II Stability in Buffers and Biological Materials ,. /. Pharm. Sci. 1989, 78,132-131. 

Pyrazolidine, 1,2-diethyl-3-hydroxymethyl-biological activity, 5, 297 Pyrazolidine, 2-ethoxycarbonyl-1 -phenyl-reactions, 5, 257 Pyrazolidine, 4-hydroxy-synthesis, 5, 155 Pyrazolidine, 1-phenyl-in Fischer indole synthesis, 5, 256 Pyrazolidine, 1 -phenyl-2-(phenylcarbamoyl)-anticonvulsant activity, 5, 297 Pyrazolidine, l-phenyl-2-thiocarbamoyl-synthesis, 5, 257... 

Data on the biological actions of dipyridothiophenes are scarce. Information is lacking in the review (1987KFZ536), where considerable attention was given to the pharmacological aspect of the use of thienopyridine derivatives. The anticonvulsive activity of substituted pyrido[3,2, 4,5]thieno[3,2-6]pyridine, which has low toxicity, was documented (1996RFP1417446). 

Depending on the composition of the various membranes, it might be appropriate to use IAM columns with different phospholipids. As these columns are not commercially available, phosphatidylcholine (PC)- or phosphatidylserine (PS)-covered infusorial earth as the stationary phase and phosphate buffer as the mobile phase have been used to determine the retention time for a series of 2,3,6-triaminopyridines with anticonvulsant activity. Again, log JCPS was superior to log K oct in describing the observed variance in biological activity [7]. 

Hamor and Lien have analyzed anticonvulsant activities of sulfamoyl-benzoates. For the test of antistrychnine activity, compounds having the same aromatic substituents are used so that no 2o-(X,Y) term appears in Equation 22. They have suggested that the similarity of equations in terms of steric, hydrophobic, and electronic properties of substituents indicates a common anticonvulsant mechanism for the two biological effects of this set of compounds. They have also suggested that the mechanism of action of these drugs was quite different from those of barbiturates and other hypnotics where quite different structure-activity correlations of physicochemical significance have been obtained. 

Pyrido[2,3-highly active compounds possessing antitumor, antibacterial, and anticonvulsive activities (80CPB761, 80JMC327, 80PHA253). 

Polyheterocyclic structures such as benzimidazoquinazoUnes 91 made up of two fused heterocyclic rings often possess potent biological activity, like antiproliferative and DNA-intercalator activity [62], antifertiUty activity [63], anticonvulsant activity, and myorelaxant activity [64]. These benzimid-azoquinazoline compounds 91 have been obtained by the condensation of... 

Shaterian and coauthors also investigated the use of PPA/SiOj for the synthesis of heterocycles containing a phthalazine moiety (Shaterian et al., 2009). Snch compounds are of great interest because they show pharmacological and biological anticonvulsant (Grasso et al., 2000), cardiotonic (Nomoto et al., 1990), and vasorelaxant (Watanabe et al., 1998) activities. 

Several substituent constants, including the Taft Eg, have been employed by Hamor and Lien in the study of anticonvulsant activities of alkyl esters of 2-sul amoylbenzoic acid against maximal electroshock and against strychnine-induced convulsions. The steric substituent constant, E, the electronic substituent constants, a and o, ana log P calculated from Hansch s ir values were examined for correlation with biological response. For antistrychnine action, the best... 

The 1,4-dihydropyridines (DHPs) classes of privileged heterocyclic pharmacophores are well known for their calcium channel blocker activity. Other versatile biological profiles of 1,4-DHPs such as anticonvulsant activity, selective adenosine-A3 receptor antagonism, radioprotective activity, sirtuin activation, and inhibition, etc. have also been well known [186]. Conventionally, 1,4-DHPs could be accessed via the Hantzsch reaction, reduction of pyridines, addition to pyridines or cycloadditions, etc. As a facile and broadly tolerable protocol, the Hantzsch reaction consisting of cyclocondensation reaction of ethyl acetoacetate (2 equivalent) with an aldehyde and ammonia remains as a frequently employed tactic for the synthesis of 1,4-DHPs in a large number of areas such as stereoselective synthesis and green chemistry [187]. 

Ethoheptazine as analgesic, 1, 167 Ethosuximide as anticonvulsant, 1, 166 Ethoxzolamide as diuretic, 1, 173 Ethylamine, o-bromophenyl-indole synthesis from, 4, 322 Ethylamine, 2-thienyl-biological activity, 4, 911 Ethylamine, 3-thienyl-biological activity, 4, 912 Ethylene... 

Methanol, l-isoquinolyl(phenyl)-confonnation, 2, 110 Methanol, pyrimidinyl-synthesis, 3, 113 Methanol, tetrahydropyran-2-yl-microwave spectra, 3, 625 Methantheline as neurotransmitter, 1, 175 therapeutic properties, 3, 882 Methaphenilene biological activity, 4, 911 Methapyrilene biological activity, 4, 911 toxicity, 4, 912 Methaqualone, 3, 150 as anticonvulsant, 1, 166 pyrido[2,3-d]pyrimidine analogues metabolism, 3, 205 as sedative, 1, 166 Metharbitone as anticonvulsant, 1, 166 Methazolamide... 

Pyrazolo[3,4-d][l,2]diazepines synthesis, 7, 597 Pyrazolop, 4- 6][ 1,4]diazepines synthesis, 5, 272 Pyrazolo[l, 4]diazepinones as anticonvulsant, 1, 170 Pyrazolo[2,3-e]diazepinones synthesis, 5, 272 1 H-Pyrazolo[l,5-6]imidazoles synthesis, 6, 992 Pyrazolo[2,3-a]imidazoles biological activity, 6, 1024 Pyrazolo[2,3-c]imidazoles reactions, 6, 1041 synthesis, 6, 1047 Pyrazolo[2,3-imidazoles synthesis, 6, 991 Pyrazolo[3,2- njisoquinolines synthesis, 5, 339 Pyrazolop, 4-c]isoquinolines synthesis, 5, 273 Pyrazolonaphthyri dines synthesis, 5, 339 Pyrazolone, diazophotolysis, 5, 252 Pyrazolone, 4,4-dihalo-rearrangements, 5, 250 Pyrazolone, ethoxy-hydrazinolysis, 5, 253 Pyrazolone, 4-halo-... 

There are similarities between the biological actions of inhalants and those of alcohol and barbiturates (Bowen et al. 1996b). For example, acute administration of inhalants affects motor coordination (Moser and Balster 1981) and induces anxiolysis, whereas chronic administration is associated with physical dependence and withdrawal (Bowen et al. 1996a Evans and Balster 1991, 1993). In addition, some inhalant drugs have anticonvulsant properties (Wood et al. 1984). Like other CNS-depressant agents, inhalants have biphasic effects on spontaneous locomotor activity in rodents, with increased activity seen at lower doses and diminished locomotion seen at higher doses (Cause et al. 1985 Kjellstrand et al. 1985). 

Additional in vivo studies on the biological activity of proanthocyani-dins investigating a series of behavioral activities (motihty, body weight gain, body temperature, motoric coordination, anticonvulsant effects and central analgesic activities) showed no or only moderate pharmacological effects [53]. On the other hand, dietary supplementation with cocoa pro-cyanidin supplements can dose-dependently prevent the development of hyperglycemia in diabetic obese mice [54]. 

Various dihydro-1,4-oxathiins and dihydro-1,4-dithiins are reported to be useful in areas other than agriculture. Thus, 2,3-dihydro-l,4-dithiin-5,6-dicarboximides display a wide spectrum of biological activity (77SST(4)332) while derivatives of the basic structure (243) have been patented as tranquilizers, anticonvulsants and hypnotics (76GEP2550163). Sedative, myorelaxant and cataleptic properties are associated with certain 2,1-benzoxathiane 2,2-dioxides (75BRP1383459). 

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