Dihydrobenzo[1,4]oxathiine: A Multi-Potent Pharmacophoric Heterocyclic Nucleus

C.      Viglianisi; S.      Menichetti

Abstract

2,3-dihydrobenzo[b][1,4]oxathiine represents a valuable pharmacophoric heterocyclic nucleus known since very long time. Initially, together with some patents reporting the use of these compounds as herbicides or lipogenesis inhibitors, several papers reported their ability as melatonin, histamine and serotonin receptor ligands, α-adrenoreceptor blockers as well as non-glycoside sweeteners. This wide range of biological activities has been recently further improved by studies stating their activity as antimycotics, multi-defense antioxidants and estrogen receptor ligands. The last insights regarding the preparation, the biological activity and the structure activity relationship (SAR) of derivatives containing the dihydrobenzoxathiine skeleton will be discussed in this review.

Keywords: 2,3-Dihydrobenzo[b][1,4]oxathiines, 4-thiaflavanes, sweeteners, antimicotic activity, multi-defense antioxidants, selective estrogen receptor modulators

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