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Prostacyclin (PGI2) scaffolds in medicinal chemistry: current and emerging drugs

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Abstract

Prostacyclin (PGI2) is a natural hormone that has primarily been explored for its potent vasodilation activity and inhibition of platelet aggregation. The chemical structure of prostacyclin has intrinsic instability in aqueous solutions that limited its analysis and clinical use. Therefore, different analogues have been designed and synthesized with similar activity as prostacyclin and with greatly improved stability. Moreover, structural modifications in its α- and ω-sidechains for some analogues resulted in better activity and/or potency and other unique functions. This review covered the discovery and chemistry of prostacyclin. The current and emerging drugs with their structural scaffolds are also reviewed herein with a detailed comparison of their structural modifications and clinical effects.

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Authors and Affiliations

  1. Department of Medicinal Chemistry and Phytochemistry, Faculty of Pharmacy, Yarmouk University, Irbid, 21163, Jordan

    Ghina’a I. Abu Deiab

  2. Department of Chemistry and Biochemistry, The University of North Carolina at Greensboro, Greensboro, NC, 27455, USA

    Mitchell P. Croatt

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  1. Ghina’a I. Abu Deiab
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Abu Deiab, G.I., Croatt, M.P. Prostacyclin (PGI2) scaffolds in medicinal chemistry: current and emerging drugs. Med Chem Res 31, 1241–1251 (2022). https://doi.org/10.1007/s00044-022-02914-x

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