Synthesis and Biological Evaluation of Amide Derivatives of (6-Chloro-2,3-dihydro-1H-inden-1-yl)acetic Acid as Potential Anti-inflammatory Agents with Lower Gastrointestinal Toxicity

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概要

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• A variety of amide derivatives of (6-chloro-2,3-dihydro-1H-inden-1-yl)acetic acid were synthesized and screened for their anti-inflammatory and related biological activities. These compounds were found to be longer acting and showed residual activity exceeding that of standard indomethacin. The studies with SKF-525A, a standard hepatic microsomal enzyme inhibitor showed that probably the test compound per se is the active species. The compound 6y showed best activity profile with ED_<30> of 6.45mg/kg however this compound was found to be toxic at 100mg/kg p.o. Though these compounds exhibited appreciable analgesic and antipyretic activities but they failed to prevent the development of secondary inflammation in adjuvant induced arthritis assay. The compound 6x showed 94% inhibition of acetic acid induced writhing. Studies showed that antagonism of TNF-α is not possibly involved in the mechanism of action of these compounds. However these compounds were found to have only mild ulcerogenic potential at the tested dose level of 100mg/kg p.o. in comparison to indomethacin.

• 公益社団法人日本薬学会の論文
• 2008-05-01

著者

• Sharma Meenakshi

  Medicinal Chemistry Research Laboratory Pharmacy Group Birla Institute Of Technology And Science

• RAY Saumendra

  Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology and Science

• Ray Saumendra

  Medicinal Chemistry Research Laboratory Pharmacy Group Birla Institute Of Technology And Science

関連論文

• Synthesis and Biological Evaluation of Amide Derivatives of (6-Chloro-2,3-dihydro-1H-inden-1-yl)acetic Acid as Potential Anti-inflammatory Agents with Lower Gastrointestinal Toxicity

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