Synthesis, pharmacological evaluation and molecular docking studies of indanone derivatives

被引：0
作者：
Ankur Patel
D. Giles
Guru Basavarajaswamy
C. Sreedhar
Avani Patel
机构：
[1] Acharya & B. M. Reddy College of Pharmacy,Department of Pharmaceutical Chemistry
来源：
Medicinal Chemistry Research | 2012年 / 21卷
关键词：
Analgesic; Anti-inflammatory; Antimicrobial; Docking; Indanone; Isoxazole;
D O I：
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中图分类号：
学科分类号：
摘要：
A new series of isoxazole fused indanones were synthesized form indane-1,3-dione. The newly synthesized derivatives were confirmed by IR, 1H NMR, and mass spectral data. The synthesized title compounds were evaluated for analgesic, anti-inflammatory, and antimicrobial activities. The modifications carried out in indanone had a positive effect in anti-inflammatory activity when compared to that of other pharmacological activities. The compounds BD6, BD7, BD9, BD10, and BD11 showed good anti-inflammatory activity when compared to that of standard indomethacin. BD3, BD4, and BD5 compounds possess moderate anti-inflammatory activity. Some compounds possess moderate analgesic and antimicrobial activity. Docking study reveals that isoxazole nucleus is essential for biological activity. It was concluded that the fusion of isoxazole with indanone nucleus will increase anti-inflammatory activity than analgesic and antimicrobial activity.
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页码：4403 / 4411
页数：8
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共 107 条
  • [1] Basappa MP(2003)Solution-phase synthesis of novel Δ Bioorg Med Chem 11 4539-4544
  • [2] Sadashiva K(2004)-isoxazoline libraries via 1,3-dipolar cycloaddition and their antifungal properties Bioorg Med Chem 14 3679-3681
  • [3] Mantelingu SN(2004)Novel δ Indian J Chem 43B 1954-1957
  • [4] Swamy KS(2007)-isoxazolines as group II phospholipase A Lett Drug Des Discov 4 49-54
  • [5] Rangappa Kumar MS(1995) inhibitors J Med Chem 38 4897-4905
  • [6] Basappa SN(2001)A simple and efficient method for the synthesis of 1,2-benzsioxazoles: a series of its potent acetylcholinesterase inhibitors Bioorg Med Chem 9 445-452
  • [7] Swamy M(2009)Synthesis and antimalarial activity of (E) 2-(2′-chloro-3′-quinolinylmethylidene)-5,7-dimethoxyindanones Eur J Med Chem 44 1210-1214
  • [8] Mahendra JS(2008)Cyclooxygenase-2 inhibitors. Synthesis and pharmacological activities of 5-methoanesulfonamido-1-indanone derivatives J Iran Chem Soc 5 67-73
  • [9] Prasad BS(1953)Positioning of the carboxamide side chain in 11- J Pharmacol Exp Ther 107 385-393
  • [10] Viswanath KS(2008)-11 Eur J Med Chem 43 1767-1773
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