title: Medicinal attributes of 1,2,3-triazoles: Current developments.
abstract: 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 NaN3under 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.
authors.affiliation: Academy of Scientific and Innovative Research (AcSIR), CSIR-IIIM, Jammu Campus, Jammu 180001, India; Bio-organic Chemistry Division, CSIR-Indian Institute of Integrative Medicine, Jammu 180001, India.
authors.forename: Divya
authors.initials: D
authors.lastname: Dheer
authors.affiliation: Department of Chemistry, National Institute of Technology (NIT), Jalandhar 144011, Punjab, India.
authors.forename: Virender
authors.initials: V
authors.lastname: Singh
authors.affiliation: Academy of Scientific and Innovative Research (AcSIR), CSIR-IIIM, Jammu Campus, Jammu 180001, India; Bio-organic Chemistry Division, CSIR-Indian Institute of Integrative Medicine, Jammu 180001, India. Electronic address: rshankar@iiim.res.in.
authors.forename: Ravi
authors.initials: R
authors.lastname: Shankar
mesh_terms: D000480:Alkynes / Q000737:chemistry; D000818:Animals; D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001386:Azides / Q000737:chemistry; D057930:Click Chemistry / Q000379:methods*; D061565:Cycloaddition Reaction / Q000379:methods; D016861:Cyclooxygenase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D055808:Drug Discovery / Q000379:methods*; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D008958:Models, Molecular; D043884:Receptor, Cannabinoid, CB1 / Q000037:antagonists & inhibitors; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000480:Alkynes; D000890:Anti-Infective Agents; D000893:Anti-Inflammatory Agents; D000970:Antineoplastic Agents; D001386:Azides; D016861:Cyclooxygenase Inhibitors; D017320:HIV Protease Inhibitors; D043884:Receptor, Cannabinoid, CB1; D014230:Triazoles
keywords: 1,2,3-Triazole; 1,3-Dipolar cycloaddition; Alkyne–azide coupling reaction; Multicomponent reaction