Synthesis and Antispasmodic Activity Evaluation of Bis-(Papaverine) Analogues

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概要

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• A new series of N-substituted bis-(tetrahydropapaverine) ring systems have been synthesised in expectation of better antispasmodic activity in comparison with papaverine. The synthesis of the targeted heterocycles is described along with a discussion of their structure activity relationship. The general synthetic methods of bis-(tetrahydropapaverine) analogues involve tetrahydropapaverine, various piperazines, diisocyanates and diisothiocyanates as starting materials. Pharmacological evaluation involves the in vitro antispasmodic activity on a freshly removed guinea pig ileum using a force displacement transducer amplifier connected to a physiograph. Among the analogues synthesized in the present study, N,N'-bis-[2-carbamoyl-1-(3,4-dimethoxybenzyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolinyl]piperazine (22), was found to be the most potent muscle relaxant (IC_<50>:0.31μM).

• 公益社団法人日本薬学会の論文
• 2004-03-01

著者

• Chandra R

  Dr. B. R. Ambedkar Centre For Biomedical Research University Of Delhi

• Ghosh Narendra

  Dr. B. R. Ambedkar Centre For Biomedical Research University Of Delhi

• KAUR Jaskiran

  Department of Chemistry, University of Pennsylvania

• CHANDRA Ramesh

  Dr. B. R. Ambedkar Centre for Biomedical Research, University of Delhi

• Kaur Jaskiran

  Department Of Chemistry University Of Pennsylvania

関連論文

• Synthesis and Antispasmodic Activity Evaluation of Bis-(Papaverine) Analogues
• Synthesis of N-Substituted Piperazinyl Carbamoyl and Acetyl Derivatives of Tetrahydropapaverine : Potent Antispasmodic Agents

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