A quantitative structure-activity study of anticonvulsant benzyl N,N-dimethylcarbamates.

Review, reevaluation, and new results in quantitative structure-activity studies of anticonvulsants

“…That is the reason for many researchers to use an indicator variable assigning the value of 1 for substituents capable of hydrogen bonding. 25 A number of (aryloxy)-aryl semicarbazones 26 were evaluated for anticonvulsant activities. The data generated from x-ray crystallography supported a binding site hypothesis and that certain interatomic distances and bond angles affected potency.…”

Application of a Stepwise Flow Ratiometry without Phase Separation to the Determination of the Chloroform/Water Distribution Coefficients of Volatile Diazines

“…Table 2 is the summary of the results obtained for the diazines. The log K D values determined by a shake flask method 9,11,15) are also listed, as reference. The log K D obtained from A S (ϭA o ϩA a ) were listed for less lipophilic compounds (log K D Ͻ1), because the addition of A o and A a is considered to give more reliable results.…”

“…Mono-and di-substituted diazines were selected as the compounds to be analyzed because their K D values in various solvents systems have been extensively explored in the studies of quantitative structure-activity relationships. [6][7][8][9][10][11] …”

Carbamate derivatives of felbamate as potential anticonvulsant agents

“…The oxygen in one of the carbamate moieties may be replaced by another atom, such as nitrogen or carbon. Limited SAR information is available for monocarbamate analogs that lack the possibility of cascade metabolic pathway to form toxic species as with felbamate (Yamagami et al, 1982;Tanaka et al, 1985). N-methyl or N,Ndimethyl substituted benzyl carbamates were more potent than unsubstituted benzyl carbamate, whereas N,N-dimethyl substitution decreases anticonvulsant activity in phenylethyl or phenylpropyl carbamates .…”