Design, synthesis, and evaluation of 2-aryl-7-(3′,4′-dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidines as novel PDE-4 inhibitors

Ikyon Kim, Jong Hwan Song, Chang Min Park, Joon Won Jeong, Hyung Rae Kim, Jin Ryul Ha, Zaesung No, Young Lan Hyun, Young Sik Cho, Nam Sook Kang, Dong Ju Jeon

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Abstract

Described herein is design, synthesis, and biological evaluation of novel series of 2-aryl-7-(3′,4′-dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidines acting as inhibitors of type 4 phosphodiesterase (PDE4) which is known as a good target for the treatment of asthma and COPD. For this purpose, structure optimization was conducted with the aid of structure-based drug design using the known X-ray crystallography. Also, biological effects of these compounds on the target enzyme were evaluated by using in vitro assays, leading to the potent and selective PDE-4 inhibitor (IC50 < 10 nM).

Original languageEnglish
Pages (from-to)922-926
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number3
DOIs
Publication statusPublished - 2010 Feb 1

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All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Cite this

Kim, I., Song, J. H., Park, C. M., Jeong, J. W., Kim, H. R., Ha, J. R., No, Z., Hyun, Y. L., Cho, Y. S., Sook Kang, N., & Jeon, D. J. (2010). Design, synthesis, and evaluation of 2-aryl-7-(3′,4′-dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidines as novel PDE-4 inhibitors. Bioorganic and Medicinal Chemistry Letters, 20(3), 922-926. https://doi.org/10.1016/j.bmcl.2009.12.070