Studies in the Heterocyclic Series. XVI. Open Azaphenothiazines as New Central Nervous System Depressants

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概要

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• Acid-catalyzed condensation of 2-amino-3-mercapto-6-methylpyridine and 3-amino-pyridine-2 [1H]-thiones with 4-chloropyrimidines having free 5-carbon centers gave N-(3-mercapto-2-pyridyl)-6-pyrimidinylamines and N-(2-thioxo-3-pyridyl)-6-pyrimidinyl-amines, which we have described as open 1,3,9-triaza- and 1,3,6-triaza-phenothiazines, respectively. A newly developed method of reducing nitro groups was used for preparing the aminopyridine precursors. Eight new and five related compounds including an open 1,9-diazaphenoxazine were tested in rats and mice and found to display central nervous system (CNS)-depressant activities. The most active compound in the series is N-(6-chloro-2 [1H]-thioxo-3-pyridyl)-2,4-diamino-6-pyrimidinylamine, an open 1,3,6-triaza-phenothiazine derivative. Structure-activity correlations are discussed on the basis of the biological data.

• 公益社団法人日本薬学会の論文
• 1982-01-25

著者

• Buckley J.p.

  Department Of Pharmacology College Of Pharmacy University Of Houston

• OKAFOR C.O.

  Department of Chemistry, University of Nigeria, Nsukka, Nigeria

• STEENBERG M.L.

  Department of Pharmacology, College of Pharmacy, University of Houston

• Steenberg M.l.

  Department Of Pharmacology College Of Pharmacy University Of Houston

• Okafor C.o.

  Department Of Chemistry University Of Nigeria Nsukka Nigeria

関連論文

• Studies in the Heterocyclic Series. XVI. Open Azaphenothiazines as New Central Nervous System Depressants

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