Literature DB >> 15013022

Discovery and SAR development of 2-(phenylamino) imidazolines as prostacyclin receptor antagonists [corrected].

Robin D Clark1, Alam Jahangir, Daniel Severance, Rick Salazar, Thomas Chang, David Chang, Mary Frances Jett, Steven Smith, Keith Bley.   

Abstract

On the basis of screening hits (1a,b), a series of selective, high affinity prostacyclin receptor antagonists was developed. The optimized lead compound 25d [(4,5-dihydro-1H-imidazol-2-yl)-[4-(4-isopropoxybenzyl)phenyl]amine] had analgesic activity in the rat.

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Year:  2004        PMID: 15013022     DOI: 10.1016/j.bmcl.2003.10.070

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


  14 in total

1.  Microsomal prostaglandin e2 synthase-1 modulates the response to vascular injury.

Authors:  Miao Wang; Kaori Ihida-Stansbury; Devashish Kothapalli; Mathieu C Tamby; Zhou Yu; Lihong Chen; Gregory Grant; Yan Cheng; John A Lawson; Richard K Assoian; Peter L Jones; Garret A Fitzgerald
Journal:  Circulation       Date:  2011-01-31       Impact factor: 29.690

2.  Inhaled iloprost suppresses the cardinal features of asthma via inhibition of airway dendritic cell function.

Authors:  Marco Idzko; Hamida Hammad; Menno van Nimwegen; Mirjam Kool; Nanda Vos; Henk C Hoogsteden; Bart N Lambrecht
Journal:  J Clin Invest       Date:  2007-02       Impact factor: 14.808

3.  Investigation of the prostacyclin (IP) receptor antagonist RO1138452 on isolated blood vessel and platelet preparations.

Authors:  R L Jones; H Wise; R Clark; R L Whiting; K R Bley
Journal:  Br J Pharmacol       Date:  2006-07-31       Impact factor: 8.739

4.  RO1138452 and RO3244794: characterization of structurally distinct, potent and selective IP (prostacyclin) receptor antagonists.

Authors:  Keith R Bley; Anindya Bhattacharya; Don V Daniels; Joel Gever; Alam Jahangir; Counde O'Yang; Steven Smith; Dinesh Srinivasan; Anthony P D W Ford; Mary-Frances Jett
Journal:  Br J Pharmacol       Date:  2006-02       Impact factor: 8.739

5.  Characterization of isoprostane signaling: evidence for a unique coordination profile of 8-iso-PGF(2alpha) with the thromboxane A(2) receptor, and activation of a separate cAMP-dependent inhibitory pathway in human platelets.

Authors:  Fadi T Khasawneh; Jin-Sheng Huang; Fozia Mir; Subhashini Srinivasan; Chinnaswamy Tiruppathi; Guy C Le Breton
Journal:  Biochem Pharmacol       Date:  2008-03-30       Impact factor: 5.858

Review 6.  Prostanoid receptor antagonists: development strategies and therapeutic applications.

Authors:  R L Jones; M A Giembycz; D F Woodward
Journal:  Br J Pharmacol       Date:  2009-07-15       Impact factor: 8.739

7.  Prostacyclin analogs stimulate receptor-mediated cAMP synthesis and ATP release from rabbit and human erythrocytes.

Authors:  Randy S Sprague; Elizabeth A Bowles; Madelyn S Hanson; Eileen A DuFaux; Meera Sridharan; Shaquria Adderley; Mary L Ellsworth; Alan H Stephenson
Journal:  Microcirculation       Date:  2008-07       Impact factor: 2.628

8.  Stimulation of fat storage by prostacyclin and selective agonists of prostanoid IP receptor during the maturation phase of cultured adipocytes.

Authors:  Ferdous Khan; Pinky Karim Syeda; Michael Nii N Nartey; Mohammad Shahidur Rahman; Mohammad Safiqul Islam; Kohji Nishimura; Mitsuo Jisaka; Fumiaki Shono; Kazushige Yokota
Journal:  Cytotechnology       Date:  2016-03-05       Impact factor: 2.058

9.  Vasorelaxation induced by prostaglandin E2 in human pulmonary vein: role of the EP4 receptor subtype.

Authors:  N Foudi; L Kotelevets; L Louedec; G Leséche; D Henin; E Chastre; X Norel
Journal:  Br J Pharmacol       Date:  2008-06-02       Impact factor: 8.739

10.  Role of cyclooxygenase isoforms in prostacyclin biosynthesis and murine prehepatic portal hypertension.

Authors:  N J Skill; N G Theodorakis; Y N Wang; J M Wu; E M Redmond; J V Sitzmann
Journal:  Am J Physiol Gastrointest Liver Physiol       Date:  2008-09-04       Impact factor: 4.052

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