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, alpha-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.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Adrenergic alpha-Antagonists / chemical synthesis
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Adrenergic alpha-Antagonists / chemistry*
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Adrenergic alpha-Antagonists / pharmacology
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Anti-Infective Agents / chemical synthesis
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Anti-Infective Agents / chemistry
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Anti-Infective Agents / pharmacology
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology
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Antioxidants / chemical synthesis
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Antioxidants / chemistry
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Antioxidants / pharmacology
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Herbicides / chemical synthesis
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Herbicides / chemistry*
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Herbicides / pharmacology
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Heterocyclic Compounds / chemistry*
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Oxathiins / chemical synthesis
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Oxathiins / chemistry*
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Oxathiins / pharmacology
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Receptors, Estrogen / chemistry
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Receptors, Estrogen / metabolism
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Sweetening Agents / chemical synthesis
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Sweetening Agents / chemistry
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Sweetening Agents / pharmacology
Substances
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Adrenergic alpha-Antagonists
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Anti-Infective Agents
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Antineoplastic Agents
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Antioxidants
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Herbicides
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Heterocyclic Compounds
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Oxathiins
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Receptors, Estrogen
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Sweetening Agents
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dihydrobenzoxathiin