| Autor: |
Misra, Radhey S., Barthwal, Jayanti P., Parmar, Surendra S., Singh, Shiva P., Stenberg, Virgil I. |
| Zdroj: |
Journal of Pharmaceutical Sciences; March 1976, Vol. 65 Issue: 3 p405-408, 4p |
| Abstrakt: |
Several 2‐(substituted alkoxy/hydrazinocarbonyl acetanilidothio)benzoxazoles/benzothiazoles were synthesized and characterized by their sharp melting points, elemental analyses, and IR spectra. All thiobenzoxazoles/benzothiazoles possessed low anticonvulsant activity, which was reflected by the 10‐40% protection afforded by these compounds against pentylenetetrazol‐induced convulsions. All thiobenzoxazoles/benzothiazoles inhibited selectively the nicotinamide adenine dinucleotide (NAD)‐dependent oxidation of pyruvate, DL‐isocitrate, and α‐ketoglutarate by rat brain homogenates. NAD‐independent oxidation of succinate remained unaltered. All 2‐(substituted hydrazinocarbonyl acetanilidothio)benzoxazoles/benzothiazoles inhibited monoamine oxidase activity of rat brain homogenates. Greater monoamine oxidase inhibition was observed with thiobenzothiazoles than with the corresponding thiobenzoxazoles. The low anticonvulsant activity possessed by these thiobenzoxazoles/benzothiazoles was found to be unrelated with their ability to inhibit cellular respiratory and monoamine oxidase activities of rat brain homogenates. |
| Databáze: |
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