-transparent.png){kind=logo}
The chemical structure and anticonvulsant activity relationship of some 5-substituted phenyl-3-pyrazolidinone derivatives were studied. Six pairs (1-hydro and 1-propyl substituted) of compounds were designed and synthesized according to the Topliss improved method, and a compound with the highest anticonvulsant activity was found, i.e. 5-(4-fluorophenyl)-1-propyl-3-pyrazolidinone, ED50 14.7 mg/kg (MES Test). QSAR analysis showed that the hydrophobic constant sigma pi greatly influenced their anticonvulsant activity, and the steric parameter (B4) and electronic parameter (I x 10(2] of the substitutions on the phenyl ring can improve the correlation coefficient (r). Smaller steric volume and more powerful electron withdrawing effect of the substitution on the 5-phenyl ring increased the anticonvulsant activity.
X P Lei, and
Y Luan, and
Y Z Ling, and
R L Li, and
Y Q Pei
January 1992,
Yao xue xue bao = Acta pharmaceutica Sinica,
X P Lei, and
Y Luan, and
Y Z Ling, and
R L Li, and
Y Q Pei
January 1988,
Yao xue xue bao = Acta pharmaceutica Sinica,
X P Lei, and
Y Luan, and
Y Z Ling, and
R L Li, and
Y Q Pei
January 1994,
Yao xue xue bao = Acta pharmaceutica Sinica,
X P Lei, and
Y Luan, and
Y Z Ling, and
R L Li, and
Y Q Pei
January 2015,
Expert opinion on drug discovery,
X P Lei, and
Y Luan, and
Y Z Ling, and
R L Li, and
Y Q Pei
January 2012,
Pharmacological reports : PR,
X P Lei, and
Y Luan, and
Y Z Ling, and
R L Li, and
Y Q Pei
January 2014,
Drug research,
X P Lei, and
Y Luan, and
Y Z Ling, and
R L Li, and
Y Q Pei
March 2007,
Bioorganic & medicinal chemistry letters,
X P Lei, and
Y Luan, and
Y Z Ling, and
R L Li, and
Y Q Pei
May 1991,
Journal of medicinal chemistry,
X P Lei, and
Y Luan, and
Y Z Ling, and
R L Li, and
Y Q Pei
March 1975,
Journal of pharmaceutical sciences,
X P Lei, and
Y Luan, and
Y Z Ling, and
R L Li, and
Y Q Pei
May 1976,
Journal of medicinal chemistry,
