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The aim of the present review is to portray a concise account of the isolation, chemistry and bioactivity of azoles-containing natural products discovered during the last few years with a special emphasis on those compounds with a new structural motif. The material will be classified on a structural basis starting from simple monocycle-containing open chain molecules to the complex polyazole-containing, medium- and large-sized macrolides. Details on the isolation procedures and on the biological targets and activities will be given. Molecules in which azoles are present as part of standard amino-acids and nucleobases will not be considered.