Literature DB >> 20634071

Synthesis and biological activity of a series of tetrasubstituted-imidazoles as P2X(7) antagonists.

Robert J Gleave1, Daryl S Walter, Paul J Beswick, Elena Fonfria, Anton D Michel, Shilina A Roman, Sac-Pham Tang.   

Abstract

A series of analogues of the pyrazole lead 1 were synthesized in which the heterocyclic core was replaced with an imidazole. A number of potent antagonists were identified and structure-activity relationships (SAR) were investigated both with respect to activity at the P2X(7) receptor and in vitro metabolic stability. Compound 10 was identified as a potent P2X(7) antagonist with reduced in vitro metabolism and high solubility. 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20634071     DOI： 10.1016/j.bmcl.2010.05.018

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


  7 in total

Review 1.  Molecular and functional properties of P2X receptors--recent progress and persisting challenges.

Authors:  Karina Kaczmarek-Hájek; Eva Lörinczi; Ralf Hausmann; Annette Nicke
Journal:  Purinergic Signal       Date:  2012-05-01       Impact factor: 3.765

Review 2.  Current advances in the synthesis and biological potencies of tri- and tetra-substituted 1H-imidazoles.

Authors:  Majid M Heravi; Mansoureh Daraie; Vahideh Zadsirjan
Journal:  Mol Divers       Date:  2015-04-12       Impact factor: 2.943

3.  Synthesis, SAR, and Pharmacological Characterization of Brain Penetrant P2X7 Receptor Antagonists.

Authors:  Brad M Savall; Duncan Wu; Meri De Angelis; Nicholas I Carruthers; Hong Ao; Qi Wang; Brian Lord; Anindya Bhattacharya; Michael A Letavic
Journal:  ACS Med Chem Lett       Date:  2015-04-24       Impact factor: 4.345

Review 4.  Transcriptional control mechanisms associated with the nucleotide receptor P2X7, a critical regulator of immunologic, osteogenic, and neurologic functions.

Authors:  Lisa Y Lenertz; Monica L Gavala; Yiming Zhu; Paul J Bertics
Journal:  Immunol Res       Date:  2011-05       Impact factor: 2.829

5.  Eco-friendly and regiospecific intramolecular cyclization reactions of cyano and carbonyl groups in N,N-disubstituted cyanamide.

Authors:  Amr H Moustafa; Walaa W Ahmed; Mohamed F Awad; Moustafa O Aboelez; Ahmed Khodairy; Amer A Amer
Journal:  Mol Divers       Date:  2022-02-27       Impact factor: 3.364

6.  Microbiological Evaluation of 4-substituted-imidazolidine Derivatives.

Authors:  M S Y Khan; A Husain; S Sharma; M Rashid
Journal:  Indian J Pharm Sci       Date:  2012-01       Impact factor: 0.975

7.  Synthesis, molecular properties, toxicity and biological evaluation of some new substituted imidazolidine derivatives in search of potent anti-inflammatory agents.

Authors:  Asif Husain; Aftab Ahmad; Shah Alam Khan; Mohd Asif; Rubina Bhutani; Fahad A Al-Abbasi
Journal:  Saudi Pharm J       Date:  2015-03-09       Impact factor: 4.330
  7 in total

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