Synthesis, pharmacological evaluation and molecular docking studies of indanone derivatives

被引：18

作者：

Patel, Ankur ^{[1
]}

Giles, D. ^{[1
]}

Basavarajaswamy, Guru ^{[1
]}

Sreedhar, C. ^{[1
]}

Patel, Avani ^{[1
]}

机构：

[1] Acharya & BM Reddy Coll Pharm, Dept Pharmaceut Chem, Bangalore 560090, Karnataka, India

来源：

MEDICINAL CHEMISTRY RESEARCH | 2012年 / 21卷 / 12期

关键词：

Analgesic; Anti-inflammatory; Antimicrobial; Docking; Indanone; Isoxazole; SIDE-CHAIN; INHIBITORS; MOIETY;

D O I：

10.1007/s00044-012-9973-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of isoxazole fused indanones were synthesized form indane-1,3-dione. The newly synthesized derivatives were confirmed by IR, H-1 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 BD (6) , BD (7) , BD (9) , BD (10) , and BD (11) showed good anti-inflammatory activity when compared to that of standard indomethacin. BD (3) , BD (4) , and BD (5) 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.

引用

页码：4403 / 4411

页数：9

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