| Literature DB >> 15351390 |
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.Entities:
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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