Literature DB >> 29197963

Synthesis and biological evaluation of imidazo[1,2-[Formula: see text]]pyridazines as inhibitors of TNF-[Formula: see text] production.

Shivaji S Pandit1, Mahesh R Kulkarni2,3, Usha Ghosh3, Yashwant B Pandit2, Nitin P Lad2,3.   

Abstract

Tumor necrosis factor-alpha (TNF-[Formula: see text] is an important pro-inflammatory cytokine responsible for a diverse range of inflammatory diseases including rheumatoid arthritis. In the present manuscript, our medicinal chemistry efforts on the design, synthesis and TNF-[Formula: see text] evaluation of a series of 3, 6-disubstituted imidazo[1,2-b]pyridazine is described. The best compounds were 3-pyridyl and (4-(methylsulfonyl)phenyl) analogs 8q and 8w, showing inhibition of TNF-[Formula: see text] production with IC[Formula: see text]values of 0.9 and 0.4 [Formula: see text]M, respectively. The identified leads have potential for further development for treatment of inflammatory diseases.

Entities:  

Keywords:  HPBMC; Imidazo[1,2-b]pyridazine; LPS; Rheumatoid arthritis; TNF-

Mesh：

Substances：

Year:  2017        PMID： 29197963     DOI： 10.1007/s11030-017-9798-8

Source DB:  PubMed          Journal:  Mol Divers        ISSN： 1381-1991            Impact factor:   2.943


  24 in total

Review 1.  Anti-TNF-alpha therapies: the next generation.

Authors:  Michael A Palladino; Frances Rena Bahjat; Emmanuel A Theodorakis; Lyle L Moldawer
Journal:  Nat Rev Drug Discov       Date:  2003-09       Impact factor: 84.694

Review 2.  The transfer of a laboratory based hypothesis to a clinically useful therapy: the development of anti-TNF therapy of rheumatoid arthritis.

Authors:  Marc Feldmann; Fionula M Brennan; Richard O Williams; James N Woody; Ravinder N Maini
Journal:  Best Pract Res Clin Rheumatol       Date:  2004-02       Impact factor: 4.098

3.  Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors.

Authors:  Emily A Peterson; Alessandro A Boezio; Paul S Andrews; Christiane M Boezio; Tammy L Bush; Alan C Cheng; Deborah Choquette; James R Coats; Adria E Colletti; Katrina W Copeland; Michelle DuPont; Russell Graceffa; Barbara Grubinska; Joseph L Kim; Richard T Lewis; Jingzhou Liu; Erin L Mullady; Michele H Potashman; Karina Romero; Paul L Shaffer; Mary K Stanton; John C Stellwagen; Yohannes Teffera; Shuyan Yi; Ti Cai; Daniel S La
Journal:  Bioorg Med Chem Lett       Date:  2012-06-16       Impact factor: 2.823

4.  Tuberculosis associated with infliximab, a tumor necrosis factor alpha-neutralizing agent.

Authors:  J Keane; S Gershon; R P Wise; E Mirabile-Levens; J Kasznica; W D Schwieterman; J N Siegel; M M Braun
Journal:  N Engl J Med       Date:  2001-10-11       Impact factor: 91.245

5.  Inhibition of allergic dermal inflammation by the novel imidazopyridazine derivative TAK-427 in a guinea pig experimental model of eczema.

Authors:  Shigeru Fukuda; Katsuo Midoro; Takayuki Kamei; Michiyo Gyoten; Yasuhiko Kawano; Yasuko Ashida; Hideaki Nagaya
Journal:  J Pharmacol Exp Ther       Date:  2002-12       Impact factor: 4.030

Review 6.  Role of cytokines in rheumatoid arthritis.

Authors:  M Feldmann; F M Brennan; R N Maini
Journal:  Annu Rev Immunol       Date:  1996       Impact factor: 28.527

7.  The role of TNF-alpha in the pathogenesis of inflammation and joint destruction in rheumatoid arthritis (RA): a study using a human RA/SCID mouse chimera.

Authors:  H Matsuno; K Yudoh; R Katayama; F Nakazawa; M Uzuki; T Sawai; T Yonezawa; Y Saeki; G S Panayi; C Pitzalis; T Kimura
Journal:  Rheumatology (Oxford)       Date:  2002-03       Impact factor: 7.580

8.  Imidazo[1,2-b]pyridazines: a potent and selective class of cyclin-dependent kinase inhibitors.

Authors:  Kate F Byth; Nicola Cooper; Janet D Culshaw; David W Heaton; Sandra E Oakes; Claire A Minshull; Richard A Norman; Richard A Pauptit; Julie A Tucker; Jason Breed; Andrew Pannifer; Siân Rowsell; Judith J Stanway; Anna L Valentine; Andrew P Thomas
Journal:  Bioorg Med Chem Lett       Date:  2004-05-03       Impact factor: 2.823

9.  Tuberculosis following the use of etanercept, a tumor necrosis factor inhibitor.

Authors:  Aparna K Mohan; Timothy R Coté; Joel A Block; Augustine M Manadan; Jeffrey N Siegel; M Miles Braun
Journal:  Clin Infect Dis       Date:  2004-07-16       Impact factor: 9.079

10.  Structural analysis identifies imidazo[1,2-b]pyridazines as PIM kinase inhibitors with in vitro antileukemic activity.

Authors:  Vanda Pogacic; Alex N Bullock; Oleg Fedorov; Panagis Filippakopoulos; Christelle Gasser; Andrea Biondi; Sandrine Meyer-Monard; Stefan Knapp; Juerg Schwaller
Journal:  Cancer Res       Date:  2007-07-15       Impact factor: 12.701
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  1 in total

1.  Cross dehydrogenative C-O coupling catalysed by a catenane-coordinated copper(i).

Authors:  Lihui Zhu; Jiasheng Li; Jun Yang; Ho Yu Au-Yeung
Journal:  Chem Sci       Date:  2020-11-01       Impact factor: 9.825
  1 in total

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