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

I Kim, JH Song, CM Park, JW Jeong, HR Kim…

Index: 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 Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 3 p. 922 - 926

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Citation Number: 31

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 ...