Quantitative Structure-Activity Relationships and Dipole Moments of Anticonvulsants and CNS Depressants

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

“…Log 1/C ϭ 0.852 log P Ϫ 0.301 log P 2 Ϫ 0.629 ϩ 4.139 (11) n ϭ 12, r ϭ 0.915, s ϭ 0.227, log P o ϭ 1.42 whereas for the same series, the MES activity was shown to be related with molecular weight (MW) 10 only.…”

“…Similarly the anti-PTZ activity of another series of miscellaneous compounds was found 10 to be related with log P and .…”

Triazole incorporated thiazoles as a new class of anticonvulsants: Design, synthesis and in vivo screening

“…The dependence of biological activity in the set of congeneric agents or lipophilic character has been shown in many types of drug action in particular, the reports by Lien and co-workers indicate that the anticonvulsant activity of different types of compounds were correlated with lipophilicity [14]. However it has been observed that the maximum potency of the drugs that act on the central nervous system (CNS) is obtained with congeners having an optimum lipophilicity (log Po).…”

Synthesis, Characterization and Anticonvulsant Activity of Some Novel 4, 5-Disubstituted-1, 2, 4-Triazole Derivatives

“…Pharmacological activity is dependent on the lipophilic character of the drug. Anticonvulsant activities of different type of compounds were correlated with lipophilicity (Lien et al, 1979).However, it has been observed that the maximum potency of the drugs which act on the central nervous system is obtained with congeners having an optimum lipophilicity (log P) near 2. In general the optimal hydrophobicity (log P≈2)of the molecules is essential for anticonvulsant activity without any neurotoxicity.…”