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Eight-membered heterocycles with two heteroatoms in a 1,5-relationship of interest in medicinal chemistry

  • Authors: Parrino B.; Cascioferro S.; Carbone D.; Cirrincione G.; Diana P.
  • Publication year: 2020
  • Type: Capitolo o Saggio
  • Key words: 1,5-Diazocines; 1,5-Dioxocins; 1,5-Dithiocins; 1,5-Oxazocines; 1,5-Thiazocines; Biological activity; Eight-membered heterocycles with two heteroatoms 1,5; Medicinal chemistry
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This review deals with 1,5-diheterocines that exhibited biological properties and covers comprehensively the literature from 2007 to the end of February 2019. Among the six possible heterocyclic systems belonging to the eight-membered rings with two heteroatoms, N, O, and S, five had derivatives showing pharmacological activities: 1,5-diazocines, 1,5-oxazocines, 1,5-thiazocines, 1,5-dioxocins, and 1,5-dithiocins. Instead, literature reported no articles dealing with 1,5-oxathiocins of interest in medicinal chemistry. In addition to uncondensed derivatives, 1,5-diheterocines fused to five- and six-membered carbocycles or heterocycles are covered. Bridged 1,5-diheterocines are covered as well.