Literature DB >> 26781932

Discovery of aminoquinazoline derivatives as human A(2A) adenosine receptor antagonists.

Gang Zhou1, Robert Aslanian2, Gioconda Gallo1, Tanweer Khan2, Rongze Kuang1, Biju Purakkattle2, Manuel De Ruiz3, Andrew Stamford1, Pauline Ting1, Heping Wu1, Hongwu Wang2, Dong Xiao2, Tao Yu1, Yonglian Zhang1, Deborra Mullins2, Robert Hodgson2.   

Abstract

Novel bicyclic adenosine A(2A) antagonists with an aminoquinazoline moiety were designed and synthesized. The optimization of the initial lead compound based on in vitro and in vivo activity has led to the discovery of a potent and selective class of adenosine A(2A) antagonists. The structure-activity relationships of this novel series of bicyclic aminoquinazoline derivatives as adenosine A(2A) antagonists are described in detail.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Adenosine A(2A) receptor antagonist; Aminoquinazoline; Parkinson’s disease

Mesh：

Substances：

Year:  2015        PMID： 26781932     DOI： 10.1016/j.bmcl.2015.11.048

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


  2 in total

1.  In Silico Studies Targeting G-protein Coupled Receptors for Drug Research Against Parkinson's Disease.

Authors:  Agostinho Lemos; Rita Melo; Antonio Jose Preto; Jose Guilherme Almeida; Irina Sousa Moreira; Maria Natalia Dias Soeiro Cordeiro
Journal:  Curr Neuropharmacol       Date:  2018       Impact factor: 7.363

2.  Discovery of Potent and Selective A2A Antagonists with Efficacy in Animal Models of Parkinson's Disease and Depression.

Authors:  Sujay Basu; Dinesh A Barawkar; Vidya Ramdas; Minakshi Naykodi; Yogesh D Shejul; Meena Patel; Sachin Thorat; Anil Panmand; K Kashinath; Rajesh Bonagiri; Vandna Prasad; Ganesh Bhat; Azfar Quraishi; Sumit Chaudhary; Amol Magdum; Ashwinkumar V Meru; Indraneel Ghosh; Ravi K Bhamidipati; Amol A Raje; Vamsi L M Madgula; Siddhartha De; Sreekanth R Rouduri; Venkata P Palle; Anita Chugh; Narayanan Hariharan; Kasim A Mookhtiar
Journal:  ACS Med Chem Lett       Date:  2017-07-05       Impact factor: 4.345
  2 in total

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