Bioorganic and Medicinal Chemistry Letters p. 3712 - 3715 (2007)
Update date:2022-08-25
Topics:
Yogeeswari, Perumal
Sriram, Dharmarajan
Sahitya, Puppala
Ragavendran, Jegadeesan Vaigunda
Ranganadh, Velagaleti
A series of pharmacophoric hybrids of ameltolide-γ-aminobutyric acid (GABA)-amides was designed, synthesized, and evaluated for their anticonvulsant and neurotoxic properties. Initial anticonvulsant screening was performed using intraperitoneal (ip) maximal electroshock-induced seizure (MES), subcutaneous pentylenetetrazole (scPTZ), and subcutaneous picrotoxin (scPIC)-induced seizure threshold tests. All the compounds had improved lipophilicity and the pharmacological activity profile confirmed their blood-brain barrier penetration. The titled compounds showed promising activity in scPIC screen indicating the involvement of GABA-mediation. Compound 4-(2-(2,6-dimethylaminophenylamino)-2-oxoethylamino)-N-(2,6-dimethylphenyl) butanamide (7) emerged as the most potent derivative effective in all the three animal models of seizure with no neurotoxicity at the anticonvulsant dose.
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