Literature DB >> 18462938

Non-acidic pyrazole EP1 receptor antagonists with in vivo analgesic efficacy.

Adrian Hall1, Andy Billinton, Susan H Brown, Nicholas M Clayton, Anita Chowdhury, Gerard M P Giblin, Paul Goldsmith, Thomas G Hayhow, David N Hurst, Ian R Kilford, Alan Naylor, Barry Passingham, Lisa Winyard.   

Abstract

Replacement of the carboxylic acid group in a series of previously described methylene-linked pyrazole EP(1) receptor antagonists led to the discovery of amide, reversed amide and carbamate derivatives. Two compounds, 10a and 10b, were identified as brain penetrant compounds and both demonstrated efficacy in the CFA model of inflammatory pain.

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Year:  2008        PMID： 18462938     DOI： 10.1016/j.bmcl.2008.04.018

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


  9 in total

1.  Synthesis and anti-HIV-1 screening of novel N'-(1-(aryl)ethylidene)-2-(5,5-dioxido-3-phenylbenzo[e]pyrazolo[4,3-c][1,2]thiazin-4(1H)-yl)acetohydrazides.

Authors:  Sana Aslam; Matloob Ahmad; Muhammad Zia-Ur-Rehman; Catherine Montero; Mervi Detorio; Masood Parvez; Raymond F Schinazi
Journal:  Arch Pharm Res       Date:  2013-07-10       Impact factor: 4.946

Review 2.  Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review.

Authors:  Khalid Karrouchi; Smaail Radi; Youssef Ramli; Jamal Taoufik; Yahia N Mabkhot; Faiz A Al-Aizari; M'hammed Ansar
Journal:  Molecules       Date:  2018-01-12       Impact factor: 4.411

3.  In vitro and in vivo characterization of PF-04418948, a novel, potent and selective prostaglandin EP₂ receptor antagonist.

Authors:  K J af Forselles; J Root; T Clarke; D Davey; K Aughton; K Dack; N Pullen
Journal:  Br J Pharmacol       Date:  2011-12       Impact factor: 8.739

4.  Development of an in vivo active, dual EP1 and EP3 selective antagonist based on a novel acyl sulfonamide bioisostere.

Authors:  Jason D Downey; Sam A Saleh; Thomas M Bridges; Ryan D Morrison; J Scott Daniels; Craig W Lindsley; Richard M Breyer
Journal:  Bioorg Med Chem Lett       Date:  2012-11-24       Impact factor: 2.823

5.  3-(4-Bromo-phen-yl)-5-[4-(dimethyl-amino)-phen-yl]-4,5-dihydro-1H-pyrazole-1-carbothio-amide.

Authors:  Hoong-Kun Fun; Thitipone Suwunwong; Suchada Chantrapromma
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-02-23

6.  Ethyl 1-cyclo-hexyl-5-(4-meth-oxy-phen-yl)-1H-pyrazole-4-carboxyl-ate.

Authors:  Hoong-Kun Fun; Ching Kheng Quah; B Chandrakantha; A M Isloor; Prakash Shetty
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-11-30

7.  Efficient Synthesis and Antimicrobial Evaluation of Pyrazolopyranopyrimidines in the Presence of SBA-Pr-SO3H as a Nanoporous Acid Catalyst.

Authors:  Ghodsi Mohammadi Ziarani; Faezeh Aleali; Negar Lashgari; Alireza Badiei; Ali Abolhasani Soorki
Journal:  Iran J Pharm Res       Date:  2018       Impact factor: 1.696

8.  (2E)-2-{[3-Methyl-5-(2-naphth-yloxy)-1-phenyl-1H-pyrazol-4-yl]methyl-idene}hydrazinecarbothio-amide monohydrate.

Authors:  Hoong-Kun Fun; Tze Shyang Chia; Shobhitha Shetty; Balakrishna Kalluraya
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-09-29

9.  3-Amino-1H-pyrazol-2-ium tri-fluoro-acetate.

Authors:  T S Yamuna; Jerry P Jasinski; Derek R Scadova; H S Yathirajan; Manpreet Kaur
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-08-14
  9 in total

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