Review Of mPGES-1 Inhibitors Based On The Benzoxazole And Its Isostere Scaffold For The Treatment Of Inflammatory Diseases

Abdullah Alwagdani

doi:10.21007/com.lsp.2024.0021

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Review Of mPGES-1 Inhibitors Based On The Benzoxazole And Its Isostere Scaffold For The Treatment Of Inflammatory Diseases

Abdullah Alwagdani·Abdullah Alwagdani

June 28, 2024DOI: 10.21007/com.lsp.2024.0021

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Abstract

The vital role of the prostanoid pathway in inflammation, pain, cancer, Alzheimer’s and many other diseases has attracted the drug discovery community to discover targets for therapeutic development. Although existing non-steroidal anti-inflammatory drugs (NSAIDs) inhibiting cyclooxygenases (COX) are widely used, the side effects of these NSAIDs limit the ling time medication. Microsomal prostaglandin E synthase-1 (mPGES-1) is an attractive target that is overexpressed during inflammations, and it could be a safe alternative to NSAIDs for treating inflammatory diseases.Since the discovery of mPGES-1 in 1997, many inhibitors have been developed since 2001. Only a few compounds were able to make it to clinical trials, and only two molecules are in phase II clinical trials. Among the mPGES-1 inhibitors, benzoxazole, indole, and benzimidazole are the most explored chemical scaffolds, especially benzimidazole. One of the two inhibitors in the clinical trials is based on this scaffold. Here, we provide a review of mPGES-1's role in inflammation and inhibitors based on these scaffolds that are reported in the literature.

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Alwagdani, A. (2024). Review Of mPGES-1 Inhibitors Based On The Benzoxazole And Its Isostere Scaffold For The Treatment Of Inflammatory Diseases. Unpublished manuscript. https://doi.org/10.21007/com.lsp.2024.0021

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Review Of mPGES-1 Inhibitors Based On The Benzoxazole And Its Isostere Scaffold For The Treatment Of Inflammatory Diseases

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