Literature DB >> 19195882

Quinolines as a novel structural class of potent and selective PDE4 inhibitors: optimisation for oral administration.

Christopher J Lunniss1, Anthony W J Cooper, Colin D Eldred, Michael Kranz, Mika Lindvall, Fiona S Lucas, Margarete Neu, Alex G S Preston, Lisa E Ranshaw, Alison J Redgrave, J Ed Robinson, Tracy J Shipley, Yemisi E Solanke, Don O Somers, Joanne O Wiseman.   

Abstract

Crystallography-driven optimisation of a lead derived from similarity searching of the GSK compound collection resulted in the discovery of a series of quinoline derivatives that were highly potent and selective inhibitors of PDE4 with a good pharmacokinetic profile in the rat. Quinolines 43 and 48 have potential as oral medicines for the treatment of COPD.

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Year:  2009        PMID： 19195882     DOI： 10.1016/j.bmcl.2009.01.045

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


  9 in total

1.  Fragment-based screening for inhibitors of PDE4A using enthalpy arrays and X-ray crystallography.

Authors:  Michael I Recht; Vandana Sridhar; John Badger; Leslie Hernandez; Barbara Chie-Leon; Vicki Nienaber; Francisco E Torres
Journal:  J Biomol Screen       Date:  2012-01-05

2.  1-[2-(4-Nitrophenyl)-5-(5-phenyl-1,2-oxazol-3-yl)-1,2,3,4-tetrahydroquinolin-4-yl]pyrrolidin-2-one.

Authors:  Margarita Gutierrez; Luis Astudillo; Luisa Quesada; Iván Brito; Matías López-Rodríguez
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-01-08

3.  Beneficial effects of quinoline-3-carboxamide (ABR-215757) on atherosclerotic plaque morphology in S100A12 transgenic ApoE null mice.

Authors:  Ling Yan; Per Bjork; Radu Butuc; Joseph Gawdzik; Judy Earley; Gene Kim; Marion A Hofmann Bowman
Journal:  Atherosclerosis       Date:  2013-02-28       Impact factor: 5.162

4.  Quinoline: A versatile heterocyclic.

Authors:  Akranth Marella; Om Prakash Tanwar; Rikta Saha; Mohammad Rahmat Ali; Sandeep Srivastava; Mymoona Akhter; Mohammad Shaquiquzzaman; Mohammad Mumtaz Alam
Journal:  Saudi Pharm J       Date:  2012-03-29       Impact factor: 4.330

5.  Repurposing human PDE4 inhibitors for neglected tropical diseases. Evaluation of analogs of the human PDE4 inhibitor GSK-256066 as inhibitors of PDEB1 of Trypanosoma brucei.

Authors:  Stefan O Ochiana; Nicholas D Bland; Luca Settimo; Robert K Campbell; Michael P Pollastri
Journal:  Chem Biol Drug Des       Date:  2014-11-18       Impact factor: 2.817

6.  Quinolinonyl Non-Diketo Acid Derivatives as Inhibitors of HIV-1 Ribonuclease H and Polymerase Functions of Reverse Transcriptase.

Authors:  Antonella Messore; Angela Corona; Valentina Noemi Madia; Francesco Saccoliti; Valeria Tudino; Alessandro De Leo; Davide Ialongo; Luigi Scipione; Daniela De Vita; Giorgio Amendola; Ettore Novellino; Sandro Cosconati; Mathieu Métifiot; Marie-Line Andreola; Francesca Esposito; Nicole Grandi; Enzo Tramontano; Roberta Costi; Roberto Di Santo
Journal:  J Med Chem       Date:  2021-06-09       Impact factor: 7.446

7.  4-Chloro-6-methyl-N-(4-methyl-phen-yl)quinolin-2-amine.

Authors:  K N Vennila; K Prabha; M Manoj; K J Rajendra Prasad; D Velmurugan
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-01-26

8.  1-[2-(4-Nitro-phen-yl)-5-(5-phenyl-1,2-oxazol-3-yl)-1,2,3,4-tetra-hydro-quinolin-4-yl]pyrrolidin-2-one monohydrate.

Authors:  Margarita Gutierrez; Gabriel Vallejos; Carlos Fernández; Alejandro Cárdenas; Iván Brito
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-12-18

9.  LPS-induced lung inflammation in marmoset monkeys - an acute model for anti-inflammatory drug testing.

Authors:  Sophie Seehase; Hans-Dieter Lauenstein; Christina Schlumbohm; Simone Switalla; Vanessa Neuhaus; Christine Förster; Hans-Gerd Fieguth; Olaf Pfennig; Eberhard Fuchs; Franz-Josef Kaup; Martina Bleyer; Jens M Hohlfeld; Armin Braun; Katherina Sewald; Sascha Knauf
Journal:  PLoS One       Date:  2012-08-28       Impact factor: 3.240
  9 in total

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