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. 2011 Jun;46(6):2236-42.
doi: 10.1016/j.ejmech.2011.03.004. Epub 2011 Mar 10.

Synthesis and anticonvulsant properties of 1-(amino-N-arylmethanethio)-3-(1-substituted benzyl-2, 3-dioxoindolin-5-yl) urea derivatives

Nadeem Siddiqui  1 , M Shamsher Alam, James P Stables
Affiliations

Synthesis and anticonvulsant properties of 1-(amino-N-arylmethanethio)-3-(1-substituted benzyl-2, 3-dioxoindolin-5-yl) urea derivatives

Nadeem Siddiqui et al. Eur J Med Chem. 2011 Jun.

Abstract

Various 1-(amino-N-arylmethanethio)-3-(1-substituted benzyl-2, 3-dioxoindolin-5-yl) urea (5a-p) were designed keeping in view the structural requirements suggested in the pharmacophore model for anticonvulsant activity. Their in vivo anticonvulsant screenings were performed by two most adopted seizure models, maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ). Compound 5f was found active in MES screening while compounds 5h, 5i, 5k and 5l showed significant anticonvulsant activity in both the screenings and were devoid of any neurotoxicity. Compound 5h and 5i showed marked protection at 300 mg/kg against MES and scPTZ screening. Compound 5i also showed protection against MES screening at the dose of 100 mg/kg. In 6 Hz screening these two compounds showed significant protection and emerged as lead compounds for future investigations.

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Figures

None
Graphical abstract
Scheme 1
Scheme 1
Synthetic route to the synthesized compounds (5a–p).
Fig. 1
Fig. 1
Anticonvulsant agents showing the required pharmacophoric elements.
See this image and copyright information in PMC

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