Literature DB >> 16962772

A novel series of imidazo[1,2-a]pyridine derivatives as HIF-1alpha prolyl hydroxylase inhibitors.

Namal C Warshakoon1, Shengde Wu, Angelique Boyer, Richard Kawamoto, Justin Sheville, Sean Renock, Kevin Xu, Matthew Pokross, Artem G Evdokimov, Richard Walter, Marlene Mekel.   

Abstract

Utilizing modeling information from a recently resolved structure of human HIF-1alpha prolyl hydroxylase (EGLN1) and structure-based design, a novel series of imidazo[1,2-a]pyridine derivatives was prepared. The activity of these compounds was determined in a human EGLN1 assay and a limited SAR was developed.

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Year:  2006        PMID： 16962772     DOI： 10.1016/j.bmcl.2006.08.089

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


  11 in total

Review 1.  Cellular oxygen sensing in health and disease.

Authors:  David R Mole; Peter J Ratcliffe
Journal:  Pediatr Nephrol       Date:  2007-10-23       Impact factor: 3.714

2.  Benzimidazole-2-pyrazole HIF Prolyl 4-Hydroxylase Inhibitors as Oral Erythropoietin Secretagogues.

Authors:  Mark D Rosen; Hariharan Venkatesan; Hillary M Peltier; Scott D Bembenek; Kimon C Kanelakis; Lucy X Zhao; Barry E Leonard; Frances M Hocutt; Xiaodong Wu; Heather L Palomino; Theresa I Brondstetter; Peter V Haugh; Laurence Cagnon; Wen Yan; Lisa A Liotta; Andrew Young; Tara Mirzadegan; Nigel P Shankley; Terrance D Barrett; Michael H Rabinowitz
Journal:  ACS Med Chem Lett       Date:  2010-10-05       Impact factor: 4.345

3.  Screening chelating inhibitors of HIF-prolyl hydroxylase domain 2 (PHD2) and factor inhibiting HIF (FIH).

Authors:  Shannon C Flagg; Cristina B Martin; Cornelius Y Taabazuing; Breanne E Holmes; Michael J Knapp
Journal:  J Inorg Biochem       Date:  2012-03-17       Impact factor: 4.155

4.  Utilization of an in vivo reporter for high throughput identification of branched small molecule regulators of hypoxic adaptation.

Authors:  Natalya A Smirnova; Ilay Rakhman; Natalia Moroz; Manuela Basso; Jimmy Payappilly; Sergey Kazakov; Francisco Hernandez-Guzman; Irina N Gaisina; Alan P Kozikowski; Rajiv R Ratan; Irina G Gazaryan
Journal:  Chem Biol       Date:  2010-04-23

5.  Fully automated continuous flow synthesis of highly functionalized imidazo[1,2-a] heterocycles.

Authors:  Ananda Herath; Russell Dahl; Nicholas D P Cosford
Journal:  Org Lett       Date:  2010-02-05       Impact factor: 6.005

6.  Reporter ligand NMR screening method for 2-oxoglutarate oxygenase inhibitors.

Authors:  Ivanhoe K H Leung; Marina Demetriades; Adam P Hardy; Clarisse Lejeune; Tristan J Smart; Andrea Szöllössi; Akane Kawamura; Christopher J Schofield; Timothy D W Claridge
Journal:  J Med Chem       Date:  2013-01-04       Impact factor: 7.446

7.  Ethyl 5-methyl-imidazo[1,2-a]pyridine-2-carboxyl-ate.

Authors:  Jin-Hua Yao; Lan-Fang Wang; Bing Guo; Kang An; Jian-Ning Guan
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-07-14

8.  N-{3-[2-(4-Fluoro-phen-oxy)eth-yl]-2,4-dioxo-1,3-diaza-spiro-[4.5]decan-7-yl}-4-methyl-benzamide.

Authors:  M Vinduvahini; Binoy Krishna Saha; H D Revanasiddappa; H C Devarajegowda
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-05-20

9.  N-{3-[2-(4-Fluoro-phen-oxy)eth-yl]-2,4-dioxo-1,3-diaza-spiro-[4.5]decan-7-yl}-4-meth-oxy-benzene-sulfonamide.

Authors:  M Vinduvahini; S Jeyaseelan; J Shylajakumari; H D Revanasiddappa; Venkatesh B Devaru
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-12-21

10.  Dual-action inhibitors of HIF prolyl hydroxylases that induce binding of a second iron ion.

Authors:  Kar Kheng Yeoh; Mun Chiang Chan; Armin Thalhammer; Marina Demetriades; Rasheduzzaman Chowdhury; Ya-Min Tian; Ineke Stolze; Luke A McNeill; Myung Kyu Lee; Esther C Y Woon; Mukram M Mackeen; Akane Kawamura; Peter J Ratcliffe; Jasmin Mecinović; Christopher J Schofield
Journal:  Org Biomol Chem       Date:  2012-11-15       Impact factor: 3.876
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