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Synthesis of Newer Indolyl/phenothiazinyl Substituted 2-oxo/thiobarbituric Acid Derivatives As Potent Anticonvulsant Agents

Overview
Specialty Pharmacology
Date 2003 Jul 12
PMID 12854356
Citations 1
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Abstract

2-Amino-5-(heteroarylmethylene)-1,3,4-oxadiazoles/thiadiazoles 7-10 were synthesized by cyclisation of 1-(heteroarylacetyl)semicarbazides/thiosemicarbazides 3-6. 5-(2'-Heteroarylmethylene-5'-aminomethylene-1',3,'4'- oxadiazol-2'-yl/thiadiazol-2'-yl)-2-oxo/thiobarbituric acids 11-18 were synthesized by condensation of compounds 7-10 at the 5th position of 2-oxo/thiobarbituric acids. The newly synthesized compounds showed anticonvulsant activity ranging from 50-90% (seizures protection). Compound 18 (5-(2'-phenothiazinylmethylene-5'-aminomethylene-1',3',4'-thiadiazol-2'- yl)-2-thiobarbituric acid) showed maximum activity being more potent than the reference drug phenytoin sodium (CAS 630-93-3).

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Liao Y, Hsu S, Chien C, Wang Y, Hsu M, Suk F Molecules. 2020; 25(12).

PMID: 32575795 PMC: 7355767. DOI: 10.3390/molecules25122856.