Substituted benzoxazole/benzthiazole-2-thiones: Interrelationship between anticonvulsant activity and inhibition of nicotinamide adenine dinucleotide-dependent oxidations and monoamine oxidase

✍ Scribed by Radhey S. Misra; Jayanti P. Barthwal; Surendra S. Parmar; Stanley J. Brumleve

• Publisher: John Wiley and Sons
• Year: 1974
• Tongue: English
• Weight: 405 KB
• Volume: 63
• Category: Article
• ISSN: 0022-3549
• DOI: 10.1002/jps.2600630318

✦ Synopsis

0 3-Alkyl benzoate/benzhydrazide aminomethyl benzoxazole/benzthiazole-2-thiones were synthesized and evaluated for their ability to affect the respiratory activity of rat brain homogenate. All compounds were found to inhibit selectively the nicotinamide adenine dinucleotide (NAD)-dependent oxidation of DL- isocitrate, a-ketoglutarate, and pyruvate while NAD-independent oxidation of succinate remained unaltered. Inhibition of monoamine oxidase by 3-benzhydrazide aminomethyl benzoxazole/ benzthiazole was greater with benzthiazoles as compared to the corresponding benzoxazoles. Anticonvulsant activity exhibited by these benzoxazole/benzthiazole derivatives against pentylenetetrazol-induced seizures was found to be unrelated to their enzyme inhibitory properties.