Substituted Piperazinoquinazolones: Relationship Between Selective Inhibition of Nicotinamide Adenine Dinucleotidedependent Oxidations and Anticonvulsant Activity
| Autor: | Stanley J. Brumleve, A.K. Chaturvedi, A. Chaudhary, Surendra S. Parmar |
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| Rok vydání: | 1974 |
| Předmět: |
Male
Isocitrates medicine.medical_treatment Hydroxybutyrates Pharmaceutical Science In Vitro Techniques Selective inhibition Nicotinamide adenine dinucleotide Piperazines Structure-Activity Relationship chemistry.chemical_compound Seizures medicine Animals ortho-Aminobenzoates Citrates Pyruvates Nicotinamide Brain NAD Rat brain Rats Concentration dependent Anticonvulsant chemistry Biochemistry Quinazolines Ketoglutaric Acids Pentylenetetrazole Anticonvulsants Pyruvic acid NAD+ kinase Oxidation-Reduction |
| Zdroj: | Journal of Pharmaceutical Sciences. 63:356-360 |
| ISSN: | 0022-3549 |
| DOI: | 10.1002/jps.2600630309 |
| Popis: | Several substituted piperazinoquinazolones were synthesized, characterized, and tested for their ability to affect the respiratory activity of rat brain homogenate. All piperazinoquinazolones were found to inhibit selectively nicotinamide adenine dinucleotide (NAD)-dependent oxidations of pyruvate, citrate, DL-isocitrate, β-hydroxybutyrate, α-ketoglutarate, and NADH while the NAD-independent oxidation of succinate remained unaltered. Inhibition of the oxidation of pyruvic acid by piperazinoquinazolones was concentration dependent, but added NAD, while stimulating the respiratory activity of brain homogenate, reduced the inhibition produced by these compounds. Some of these piperazinoquinazolones possessed anticonvulsant activity; however, this activity was found to be unrelated to their ability to inhibit the respiratory activity of the rat brain homogenate. |
| Databáze: | OpenAIRE |
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