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

Research output: Contribution to journalArticle

45 Citations (Scopus)

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

Fingerprint

Phosphodiesterase 4 Inhibitors
Drug Design
X ray crystallography
X Ray Crystallography
Chronic Obstructive Pulmonary Disease
Inhibitory Concentration 50
Assays
Asthma
Enzymes
Pharmaceutical Preparations
pyrazolo(1,5-a)pyrimidine
In Vitro Techniques

All Science Journal Classification (ASJC) codes

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

Cite this

Kim, Ikyon ; Song, Jong Hwan ; Park, Chang Min ; Jeong, Joon Won ; Kim, Hyung Rae ; Ha, Jin Ryul ; No, Zaesung ; Hyun, Young Lan ; Cho, Young Sik ; Sook Kang, Nam ; Jeon, Dong Ju. / Design, synthesis, and evaluation of 2-aryl-7-(3′,4′-dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidines as novel PDE-4 inhibitors. In: Bioorganic and Medicinal Chemistry Letters. 2010 ; Vol. 20, No. 3. pp. 922-926.
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Design, synthesis, and evaluation of 2-aryl-7-(3′,4′-dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidines as novel PDE-4 inhibitors. / Kim, Ikyon; Song, Jong Hwan; Park, Chang Min; Jeong, Joon Won; Kim, Hyung Rae; Ha, Jin Ryul; No, Zaesung; Hyun, Young Lan; Cho, Young Sik; Sook Kang, Nam; Jeon, Dong Ju.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 20, No. 3, 01.02.2010, p. 922-926.

Research output: Contribution to journalArticle

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AU - Park, Chang Min

AU - Jeong, Joon Won

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AU - Ha, Jin Ryul

AU - No, Zaesung

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AU - Sook Kang, Nam

AU - Jeon, Dong Ju

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