Literature DB >> 19447034

Discovery of selective PDE4B inhibitors.

Kenji Naganuma1, Akifumi Omura, Naomi Maekawara, Masahiro Saitoh, Naoto Ohkawa, Takashi Kubota, Hiromitsu Nagumo, Toshiyuki Kodama, Masayoshi Takemura, Yuji Ohtsuka, Junji Nakamura, Ryuichi Tsujita, Koh Kawasaki, Hirotsugu Yokoi, Masashi Kawanishi.   

Abstract

In this study the first PDE4B selective inhibitor is described. Optimization of lead 2-arylpyrimidine derivatives afforded a series of potent PDE4B inhibitors with >100-fold selectivity over the PDE4D isozyme. With a good pharmacokinetic profile, a selected compound exhibited potent anti-inflammatory effects in vivo and showed less emesis compared with Cilomilast.

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Year:  2009        PMID: 19447034     DOI: 10.1016/j.bmcl.2009.04.121

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  28 in total

1.  New insights into PDE4B inhibitor selectivity: CoMFA analyses and molecular docking studies.

Authors:  Sara Guariento; Olga Bruno; Paola Fossa; Elena Cichero
Journal:  Mol Divers       Date:  2015-08-20       Impact factor: 2.943

Review 2.  PDE4 as a target for cognition enhancement.

Authors:  Wito Richter; Frank S Menniti; Han-Ting Zhang; Marco Conti
Journal:  Expert Opin Ther Targets       Date:  2013-07-25       Impact factor: 6.902

3.  Phosphodiesterase 4B is essential for T(H)2-cell function and development of airway hyperresponsiveness in allergic asthma.

Authors:  S-L Catherine Jin; Sho Goya; Susumu Nakae; Dan Wang; Matthew Bruss; Chiaoyin Hou; Dale Umetsu; Marco Conti
Journal:  J Allergy Clin Immunol       Date:  2010-11-03       Impact factor: 10.793

Review 4.  The Gewald multicomponent reaction.

Authors:  Yijun Huang; Alexander Dömling
Journal:  Mol Divers       Date:  2010-02-27       Impact factor: 2.943

5.  Phosphodiesterase 4 inhibitors and drugs of abuse: current knowledge and therapeutic opportunities.

Authors:  Christopher M Olsen; Qing-Song Liu
Journal:  Front Biol (Beijing)       Date:  2016-10-17

Review 6.  Phosphodiesterase-4 (PDE4) molecular pharmacology and Alzheimer's disease.

Authors:  Mark E Gurney; Emily C D'Amato; Alex B Burgin
Journal:  Neurotherapeutics       Date:  2015-01       Impact factor: 7.620

7.  Ferulic acid prevents LPS-induced up-regulation of PDE4B and stimulates the cAMP/CREB signaling pathway in PC12 cells.

Authors:  Hao Huang; Qian Hong; Hong-Ling Tan; Cheng-Rong Xiao; Yue Gao
Journal:  Acta Pharmacol Sin       Date:  2016-09-26       Impact factor: 6.150

8.  Discovery of triazines as selective PDE4B versus PDE4D inhibitors.

Authors:  Timothy J Hagen; Xuesheng Mo; Alex B Burgin; David Fox; Zheng Zhang; Mark E Gurney
Journal:  Bioorg Med Chem Lett       Date:  2014-06-12       Impact factor: 2.823

9.  Structural basis for the design of selective phosphodiesterase 4B inhibitors.

Authors:  David Fox; Alex B Burgin; Mark E Gurney
Journal:  Cell Signal       Date:  2013-12-19       Impact factor: 4.315

Review 10.  PDE4 subtypes in cancer.

Authors:  Samuel Hsien Lai; Guston Zervoudakis; Jesse Chou; Mark E Gurney; Kelly M Quesnelle
Journal:  Oncogene       Date:  2020-03-20       Impact factor: 9.867

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