药效团                        
                
                                
                        
                            化学                        
                
                                
                        
                            组合化学                        
                
                                
                        
                            点击化学                        
                
                                
                        
                            氰化                        
                
                                
                        
                            生物甾体                        
                
                                
                        
                            药物发现                        
                
                                
                        
                            立体化学                        
                
                                
                        
                            有机化学                        
                
                                
                        
                            化学合成                        
                
                                
                        
                            生物化学                        
                
                                
                        
                            催化作用                        
                
                                
                        
                            体外                        
                
                        
                    
            作者
            
                Divya Dheer,Virender Singh,Ravi Shankar            
         
                    
        
    
            
            标识
            
                                    DOI:10.1016/j.bioorg.2017.01.010
                                    
                                
                                 
         
        
                
            摘要
            
            1,2,3-Triazoles are important five-membered heterocyclic scaffold due to their extensive biological activities. This framework can be readily obtained in good to excellent yields on the multigram scale through click chemistry via reaction of aryl/alkyl halides, alkynes and NaN3 under ambient conditions. It has been an emerging area of interest for many researchers throughout the globe owing to its immense pharmacological scope. The present work aims to summarize the current approaches adopted for the synthesis of the 1,2,3-triazole and medicinal significance of these architectures as a lead structure for the discovery of drug molecules such as COX-1/COX-2 inhibitors (celecoxib, pyrazofurin), HIV protease inhibitors, CB1 cannabinoid receptor antagonist and much more which are in the pipeline of clinical trials. The emphasis has been given on the major advancements in the medicinal prospectus of this pharmacophore for the period during 2008-2016.
         
            
 
                 
                
                    
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