Paper
Synthesis and Activity Evaluation of Some Novel Derivatives of 4,5,6,7-Tetrahydrothieno [3,2-c]-Pyridine Containing Substituted Piperazine or Piperidine
Published Jan 1, 2009 · C. Die
The Chinese Pharmaceutical Journal
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Abstract
OBJECTIVE To design and synthesize a novel series of 4,5,6,7-tetrahydrothieno [3,2-c] pyridine containing substituted piperazine or piperidine derivatives and to test their in vivo anti-platelet aggregation activity in the rat. METHODS Key intermediate 2 was synthesized by connecting compound 1 with chloroacetyl chloride. Title compounds 3-19 were produced by connecting intermediate 2 with a series of substituted piperazine or piperidine. RESULTS 17 novel compounds were synthesized and structurally characterized by 1H NMR and MS. Their in vivo anti-platelet aggregation activities were evaluated in the rat. Compounds 10-14 exhibited more potent inhibitory activity than other compounds synthesized. CONCLUSION These thienopyridine derivatives showed a certain anti-platelet aggregation activity,and were worth further developing as promising lead compounds.
Novel 4,5,6,7-tetrahydrothieno [3,2-c] pyridine derivatives with substituted piperazine or piperidine show promising anti-platelet aggregation activity, warranting further development as promising lead compounds.
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