Design,synthesis, and evaluation of 2-aryl-7-(3′,4′-dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidines as novel PDE-4 inhibitors |
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| Authors: | 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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| Institution: | 1. Medicinal Chemistry Research Center, Korea Research Institute of Chemical Technology, Daejeon 305-600, Republic of Korea;2. Institut Pasteur Korea, Sampyeong-dong 696, Bundang-gu, Seongnam-si, Gyeonggi-do, Republic of Korea;3. Crystalgenomics, Inc. Seoul 138-736, Republic of Korea;4. Pharmacology Research Center, Korea Research Institute of Chemical Technology, Daejeon 305-600, Republic of Korea;5. Drug Discovery Platform Technology Team, Korea Research Institute of Chemical Technology, Daejeon 305-600, Republic of Korea |
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| Abstract: | Described herein is design, synthesis, and biological evaluation of novel series of 2-aryl-7-(3′,4′-dialkoxyphenyl)-pyrazolo1,5-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). |
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