| Summary: | A phytochemical investigation on the whole plants of <i>Aerides multiflora</i> revealed the presence of three new biphenanthrene derivatives named aerimultins A–C (<b>1</b>–<b>3</b>) and a new natural phenylpropanoid ester dihydrosinapyl dihydroferulate (<b>4</b>), together with six known compounds (<b>5–10</b>). The structures of the new compounds were elucidated by analysis of their spectroscopic data. All of the isolates were evaluated for their <i>a</i>-glucosidase inhibitory activity. Aerimultin C (<b>3</b>) showed the most potent activity. The other compounds, except for compound <b>4</b>, also exhibited stronger activity than the positive control acarbose. Compound <b>3</b> showed non-competitive inhibition of the enzyme as determined from a Lineweaver–Burk plot. This study is the first phytochemical and biological investigation of <i>A. multiflora</i>.
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