Literature DB >> 18243697

Identification of a potent new chemotype for the selective inhibition of PDE4.

Amanda P Skoumbourdis1, Ruili Huang, Noel Southall, William Leister, Vicky Guo, Ming-Hsuang Cho, James Inglese, Marshall Nirenberg, Christopher P Austin, Menghang Xia, Craig J Thomas.   

Abstract

A series of substituted 3,6-diphenyl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines were prepared and analyzed as inhibitors of phosphodiesterase 4 (PDE4). Synthesis, structure-activity relationships, and the selectivity of a highly potent analogue against related phosphodiesterase isoforms are presented.

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Year:  2008        PMID： 18243697      PMCID： PMC2268978          DOI： 10.1016/j.bmcl.2008.01.028

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


  23 in total

Review 1.  Immunosuppressive and anti-inflammatory effects of cyclic AMP phosphodiesterase (PDE) type 4 inhibitors.

Authors:  J E Souness; D Aldous; C Sargent
Journal:  Immunopharmacology       Date:  2000-05

Review 2.  Phosphodiesterase-4 as a potential drug target.

Authors:  Kam Y J Zhang; Prabha N Ibrahim; Sam Gillette; Gideon Bollag
Journal:  Expert Opin Ther Targets       Date:  2005-12       Impact factor: 6.902

3.  Novel 5,6-dihydropyrazolo[3,4-E][1,4]diazepin-4 (1H)-one derivatives for the treatment of asthma and chronic obstructive pulmonary disease.

Authors:  Hazel J Dyke
Journal:  Expert Opin Ther Pat       Date:  2007-09       Impact factor: 6.674

4.  The effect of selective and non-selective phosphodiesterase inhibitors on allergen- and leukotriene C(4)-induced contractions in passively sensitized human airways.

Authors:  D T Schmidt; N Watson; G Dent; E Rühlmann; D Branscheid; H Magnussen; K F Rabe
Journal:  Br J Pharmacol       Date:  2000-12       Impact factor: 8.739

5.  Atomic structure of PDE4: insights into phosphodiesterase mechanism and specificity.

Authors:  R X Xu; A M Hassell; D Vanderwall; M H Lambert; W D Holmes; M A Luther; W J Rocque; M V Milburn; Y Zhao; H Ke; R T Nolte
Journal:  Science       Date:  2000-06-09       Impact factor: 47.728

Review 6.  Targeting the CREB pathway for memory enhancers.

Authors:  Tim Tully; Rusiko Bourtchouladze; Rod Scott; John Tallman
Journal:  Nat Rev Drug Discov       Date:  2003-04       Impact factor: 84.694

Review 7.  Phosphodiesterase-4 inhibitors as a novel approach for the treatment of respiratory disease: cilomilast.

Authors:  Claus Kroegel; Martin Foerster
Journal:  Expert Opin Investig Drugs       Date:  2007-01       Impact factor: 6.206

8.  Suppression of human inflammatory cell function by subtype-selective PDE4 inhibitors correlates with inhibition of PDE4A and PDE4B.

Authors:  C D Manning; M Burman; S B Christensen; L B Cieslinski; D M Essayan; M Grous; T J Torphy; M S Barnette
Journal:  Br J Pharmacol       Date:  1999-12       Impact factor: 8.739

Review 9.  What turns CREB on?

Authors:  Mona Johannessen; Marit Pedersen Delghandi; Ugo Moens
Journal:  Cell Signal       Date:  2004-11       Impact factor: 4.315

10.  Anxiogenic-like behavioral phenotype of mice deficient in phosphodiesterase 4B (PDE4B).

Authors:  Han-Ting Zhang; Ying Huang; Anbrin Masood; Lisa R Stolinski; Yunfeng Li; Lei Zhang; Daniel Dlaboga; S-L Catherine Jin; Marco Conti; James M O'Donnell
Journal:  Neuropsychopharmacology       Date:  2007-08-15       Impact factor: 7.853
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  6 in total

Review 1.  NIMH initiatives to facilitate collaborations among industry, academia, and government for the discovery and clinical testing of novel models and drugs for psychiatric disorders.

Authors:  Linda S Brady; Lois Winsky; Wayne Goodman; Mary Ellen Oliveri; Ellen Stover
Journal:  Neuropsychopharmacology       Date:  2008-09-17       Impact factor: 7.853

2.  A cell-based PDE4 assay in 1536-well plate format for high-throughput screening.

Authors:  Steven A Titus; Xiao Li; Noel Southall; Jianming Lu; James Inglese; Michael Brasch; Christopher P Austin; Wei Zheng
Journal:  J Biomol Screen       Date:  2008-06-30

Review 3.  The pilot phase of the NIH Chemical Genomics Center.

Authors:  Craig J Thomas; Douglas S Auld; Ruili Huang; Wenwei Huang; Ajit Jadhav; Ronald L Johnson; William Leister; David J Maloney; Juan J Marugan; Sam Michael; Anton Simeonov; Noel Southall; Menghang Xia; Wei Zheng; James Inglese; Christopher P Austin
Journal:  Curr Top Med Chem       Date:  2009       Impact factor: 3.295

4.  Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.

Authors:  Amanda P Skoumbourdis; Christopher A Leclair; Eduard Stefan; Adrian G Turjanski; William Maguire; Steven A Titus; Ruili Huang; Douglas S Auld; James Inglese; Christopher P Austin; Stephen W Michnick; Menghang Xia; Craig J Thomas
Journal:  Bioorg Med Chem Lett       Date:  2009-01-23       Impact factor: 2.823

5.  Identification of compounds that potentiate CREB signaling as possible enhancers of long-term memory.

Authors:  Menghang Xia; Ruili Huang; Vicky Guo; Noel Southall; Ming-Hsuang Cho; James Inglese; Christopher P Austin; Marshall Nirenberg
Journal:  Proc Natl Acad Sci U S A       Date:  2009-02-05       Impact factor: 11.205

6.  The reaction of ethyl 2-oxo-2H-chromene-3-carboxylate with hydrazine hydrate.

Authors:  Hatem A Abdel-Aziz; Tilal Elsaman; Mohamed I Attia; Amer M Alanazi
Journal:  Molecules       Date:  2013-02-06       Impact factor: 4.411
  6 in total

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