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Bioorganic & medicinal chemistry letters. 2020 Aug 15;30(16):127337. doi: 10.1016/j.bmcl.2020.127337 Q22.22025

Design and synthesis of pyrazolo[3,4-d]pyrimidinone derivatives: Discovery of selective phosphodiesterase-5 inhibitors

吡唑并[3,4-D]嘧啶酮衍生物的设计合成及选择性磷酸二酯酶-5抑制剂的发现 翻译改进

Mohamed A Shaaban  1, Yaseen A M M Elshaier  2, Ali H Hammad  3, Nahla A Farag  4, Haredy Hassan Haredy  5, Ahmed A AbdEl-Ghany  6, Khaled O Mohamed  7

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作者单位

  • 1 Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, 11562, Egypt.
  • 2 Organic & Medicinal Chemistry Department, Faculty of Pharmacy, University of Sadat City, Sadat City, Menoufia, 32958, Egypt. Electronic address: yaseenelshaier@azher.edu.eg.
  • 3 Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy (Boys), Al-Azahar University, Cairo 11884, Egypt.
  • 4 Pharmaceutical Chemistry Department, Faculty of Pharmacy, Misr International University, Cairo 11431, Egypt.
  • 5 Department of Pharmacology, Faculty of Medicine, Al-Azher University, 71524 Assiut, Egypt.
  • 6 Biochemistry Department, Faculty of Pharmacy, Al-Azher University, 71524 Assiut, Egypt; Biochemistry Department, Faculty of Pharmacy, Nahda University, Benisuif, Egypt.
  • 7 Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, 11562, Egypt. Electronic address: khaled.mohamed@pharma.cu.edu.eg.

    • DOI: 10.1016/j.bmcl.2020.127337 PMID: 32631538

    摘要 Ai翻译

    A novel series of 1,6-disubstituted pyrazolo[3,4-d]pyrimidin-7-one derivatives, 2a-h, 4a-d, 5 and 6, were successfully synthesized, which showed promising, and potent inhibition of phosphodiesterase 5 (PDE5). The inhibitory activities of 5, 4b, 2a, 2d, 2f, 4d and 4a against PDE5 were similar to that of sildenafil (100%). These compounds exhibited potent relaxant effects on isolated rat cavernosum tissue with pEC50 values ranging from 8.31 to 5.16 µM. Pyrazolo[3,4-d]pyrimidin-7-one scaffolds have been rationally designed via consecutive molecular modelling studies prior to their synthesis and biological evaluation. In addition, the results of the pharmacophore-based virtual screening revealed that 1v0p_PVB might have promising activity as a PDE-5 inhibitor.

    Keywords: Cavernosum tissue; Molecular modelling; PDE-5 inhibitors; Phosphodiesterase 5 (PDE5); Pyrazolo[3,4-d]pyrimidin-7-one; Sildenafil.

    Keywords：phosphodiesterase-5 inhibitors

    关键词：吡唑并嘧啶酮衍生物; 磷酸二酯酶-5抑制剂

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    期刊名：Bioorganic & medicinal chemistry letters

    缩写：BIOORG MED CHEM LETT

    ISSN：0960-894X

    e-ISSN：1464-3405

    IF/分区：2.2/Q2

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    Design and synthesis of pyrazolo[3,4-d]pyrimidinone derivatives: Discovery of selective phosphodiesterase-5 inhibitors