Current Bioactive Compounds

Adriano Mollica
Department of Pharmacy, University ”G. d' Annunzio” of Chieti-Pescara
Via dei Vestini 31
Chieti, 66100


A Recent Portrait of Bioactive Triazoles

Author(s): I. Pibiri, S. Buscemi.


Scientists have extensively explored new synthetic routes in order to obtain 1,2,3- and 1,2,4-triazoles as they represent a very interesting class of compounds due to their wide range of biological activities such as antitumor, antiinflammatory, analgesic, antifungal, antibacterial, antiviral, etc. This mini review reports the synthesis and the biological activities of compounds containing a triazole moiety published since 2007. No attempt is made to provide a comprehensive literature overview, our aim is to highlight some more recent examples of synthetic biological active compounds. In particular, we focus on the applications of “click reactions” that allow the regioselective synthesis of 1,2,3 triazoles as well as on bioactive 1,2,4 triazoles obtained by classic and improved synthetic methodologies. Moreover bioactivity of glycoconjugated, and metal complexes with triazole as ligands are herein discussed, fused ring heterocycles have not been taken into account. Where possible some comments on structure-activity relationships are referred.

Keywords: Antibacterial, antifungal, antitumor, antiviral, click reaction, enzyme-inhibitor, triazole, tazobactam, cancer chemotherapy, Carboxyamidotriazole (CAI), Ribavirin, Anastrozole, letrozole, vorozole, alprazolam, estazolam, trazodon, etoperidone, efazodone, Copper Catalyzed Azide-Alkyne Cycloadditions (CuAAC), Huisgen cycloaddition, Strobilurin A, Azoxystrobin, seed germination assay, Raphanus sativus, Staphylococcus aureus, erythromycin, Trypanosoma cruzi, bovine aortic endothelial cells, BAECs, radiolabeling, Carbonic Anhydrase Inhibitors, Tyrosine Kinase Inhibitors, MDA-MB-453, MTT Assay, Western blot Assay, Chitinase Inhibitors, Serratia marcescens, anti-160, COX-2, naproxen, Flurbiprofen, GI safety profile, indomethacin, writhing test, aspirin, Candida krusei, Candida albicans, Candida parapsilosis, Carrageenan-Induced Paw Edema, Broth Microdilution Test, penicillin zone, Escherichia coli, Bacillus subtilis, Aspergillus niger, Cryptococcus neoformans, C. neoformans, Plasmodium falciparum, bifonazole, Gibberella zeae, Colletotrichum orbiculare, Streptococcus pyogenes, Pseudomonas aeruginosa (PA), Salmonella typhi, Aspergillus flavus, Cladosporium, Combretastatin A-4, Combretum caffrum, Ruthenium(III), NNRTIs

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Article Details

Year: 2010
Page: [208 - 242]
Pages: 35
DOI: 10.2174/157340710793237281
Price: $58