Abstract
This letter describes the total synthesis, preliminary biological evaluation and mechanism studies of a novel and structurally unique isochromanone, (+/-)7,8-dihydroxy-3-methyl-isochromanone-4 (1), a nature product contained in banana (Musa sapientum L.) peel. The bioassay showed that compound 1 displays potent antihypertensive activity in renal hypertensive rats and further mechanism studies revealed that it is an ACE inhibitor.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Angiotensin-Converting Enzyme Inhibitors / chemistry*
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Angiotensin-Converting Enzyme Inhibitors / pharmacology
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Animals
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Antihypertensive Agents / chemistry*
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Antihypertensive Agents / pharmacology
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Chemistry, Pharmaceutical / methods*
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Chromones / chemistry*
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Chromones / pharmacology
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Drug Design
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Hypertension, Renal / drug therapy*
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Hypertension, Renal / metabolism
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Liver / drug effects
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Models, Chemical
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Molecular Structure
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Musa / metabolism
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Plant Extracts / pharmacology
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Rats
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Structure-Activity Relationship
Substances
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7,8-dihydroxy-3-methyl-isochromanone-4
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Angiotensin-Converting Enzyme Inhibitors
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Antihypertensive Agents
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Chromones
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Plant Extracts