Literature DB >> 15351390

Design, synthesis, and biological evaluation of new phosphodiesterase type 4 inhibitors.

Hiroshi Ochiai1, Yoshihiko Odagaki, Tazumi Ohtani, Akiharu Ishida, Kensuke Kusumi, Katuya Kishikawa, Susumu Yamamoto, Hiroshi Takeda, Takaaki Obata, Kaoru Kobayashi, Hisao Nakai, Masaaki Toda.   

Abstract

The design, synthesis, and biological evaluation of new phosphodiesterase type 4 inhibitors, which possess new templates instead of a cyclohexane ring, are described. The mode of interaction with the enzyme is discussed based on the structure-activity relationship (SAR) data obtained for the synthesized inhibitors. Furthermore, the roles of three pharmacophores, a catechol moiety, a nitrile moiety, and acidic moieties, are discussed using in silico docking studies. More detailed biological evaluations of selected compounds are also presented.

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Year:  2004        PMID: 15351390     DOI: 10.1016/j.bmc.2004.07.040

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  1 in total

1.  Pharmacophore modeling and virtual screening for the discovery of new type 4 cAMP phosphodiesterase (PDE4) inhibitors.

Authors:  Miaomiao Niu; Fenggong Dong; Shi Tang; Guissi Fida; Jingyi Qin; Jiadan Qiu; Kangbo Liu; Weidong Gao; Yueqing Gu
Journal:  PLoS One       Date:  2013-12-10       Impact factor: 3.240

  1 in total

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