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Review
. 2022 Jun;12(6):2790-2807.
doi: 10.1016/j.apsb.2022.01.002. Epub 2022 Jan 11.

Recent development on COX-2 inhibitors as promising anti-inflammatory agents: The past 10 years

Zhiran Ju  1   2 , Menglan Li  1 , Junde Xu  1 , Daniel C Howell  1 , Zhiyun Li  1 , Fen-Er Chen  1   3   4
Affiliations
Review

Recent development on COX-2 inhibitors as promising anti-inflammatory agents: The past 10 years

Zhiran Ju et al. Acta Pharm Sin B. 2022 Jun.

Abstract

Cyclooxygenases play a vital role in inflammation and are responsible for the production of prostaglandins. Two cyclooxygenases are described, the constitutive cyclooxygenase-1 and the inducible cyclooxygenase-2, for which the target inhibitors are the non-steroidal anti-inflammatory drugs (NSAIDs). Prostaglandins are a class of lipid compounds that mediate acute and chronic inflammation. NSAIDs are the most frequent choices for treatment of inflammation. Nevertheless, currently used anti-inflammatory drugs have become associated with a variety of adverse effects which lead to diminished output even market withdrawal. Recently, more studies have been carried out on searching novel selective COX-2 inhibitors with safety profiles. In this review, we highlight the various structural classes of organic and natural scaffolds with efficient COX-2 inhibitory activity reported during 2011-2021. It will be valuable for pharmaceutical scientists to read up on the current chemicals to pave the way for subsequent research.

Keywords: Adverse effects; COX-2 inhibitors; Cyclooxygenase; Inflammation; Prostaglandins.

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Figures

Image 1
Graphical abstract
Figure 1
Figure 1
Structure formulas of clinically used COX-1 and COX-2 inhibitors.
Figure 2
Figure 2
A diagram of the biochemistry of prostanoids.
Figure 3
Figure 3
A diagram of the putative anti-inflammatory mechanism of the COX-2 inhibitor in RAW264.7 cells.
Figure 4
Figure 4
Chemical structures of compounds 1–16.
Figure 5
Figure 5
Chemical structures of compounds 17–25.
Figure 6
Figure 6
Chemical structures of compounds 26–33.
Figure 7
Figure 7
Chemical structures of compounds 34–38.
Figure 8
Figure 8
Chemical structures of compounds 39–48.
Figure 9
Figure 9
Chemical structures of compounds 49–55.
Figure 10
Figure 10
Chemical structures of compounds 56–70.
Figure 11
Figure 11
Chemical structures of compounds 71–79.
Figure 12
Figure 12
Chemical structures of compounds 80–94.
Figure 13
Figure 13
Chemical structures of compounds 95–99.
Figure 14
Figure 14
Chemical structures of compounds 100–111.
Figure 15
Figure 15
Chemical structures of compounds 112–123.
Figure 16
Figure 16
Chemical structures of compounds 124–143.
Figure 17
Figure 17
Chemical structures of compounds 144-160.
Figure 18
Figure 18
Chemical structures of compounds 161–166.
Figure 19
Figure 19
Chemical structures of compounds 167–176.
See this image and copyright information in PMC

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