Pyrazolone Derivatives : Synthesis, Anti-inflammatory, Analgesic, Quantitative Structure-Activity Relationship and in Vitro Studies
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- Ragab Fatma Abdel-Fattah
- Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University
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- Abdel-Gawad Nagwa Mohamed
- Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University
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- Georgey Hanan Hanna
- Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University
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- Said Mona Fikry
- Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University
書誌事項
- タイトル別名
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- Pyrazolone Derivatives: Synthesis, Anti-inflammatory, Analgesic, Quantitative Structure–Activity Relationship and <i>in Vitro</i> Studies
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抄録
Some 1-(4-chlorophenyl or benzenesulfonamide)-2,3- and/or 4-substituted-1H-pyrazol-5(4H)-one derivatives were synthesized and screened for their anti-inflammatory and analgesic activities, in addition to their ulcerogenic liability. They were found to be active as anti-inflammatory and analgesic agents. Compound 6b was found to be the most active as anti-inflammatory agent and compound 9b was found to be the most active one as anti-inflammatory and analgesic agent. On the other hand, cyclooxygenase-1/-2 (COX-1)/COX-2 isozyme selectivity was also done and the tested compounds showed equal inhibition to both isoforms. Moreover, 2D-quantitative structure–activity relationship (QSAR) studies revealed well predictive and statistically significant and cross validated QSAR model that helps to explore some expectedly potent compounds.
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 61 (8), 834-845, 2013
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390001204178322048
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- NII論文ID
- 130003360815
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- NII書誌ID
- AA00602100
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- COI
- 1:STN:280:DC%2BC3sflslWjtQ%3D%3D
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 024715343
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- PubMed
- 23902866
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可