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The synthesis of (N-substituted)amino-spiroalkan-dione derivatives 3 is described starting from enamines 1 and carbon suboxide 2, and their inhibitory effects on blood coagulation in vivo and on platelet aggregation in vitro are determined. Some of synthesized compounds showed a strong anticoagulant activity. A comparative pharmacological study of the anticoagulant effects of the new compounds versus Warfarin suggests that their behaviour is analogous, though the action mechanism is different.

Bioactivity-guided fractionation of the methanol extract from the leaves of Santolina insularis led to the isolation of one new xanthone, (E)-3-{6-[(E)-3-hydroxy-3-oxo-1-propenyl]-9- oxo-9H-xanthen-2-yl}-2-propenoic acid, together with six known flavonoids: hispidulin, nepetin, cirsimaritin, rhamnocitrin, luteolin and luteolin 7-O-β-ᴅ-glucopyranoside. The structures were elucidated by means of 1D-, 2D-NMR spectroscopy and mass spectrometry. The topical anti-inflammatory activity of all isolated compounds and extracts was investigated employing the croton oil-induced dermatitis in mouse ear. The most active compound, luteolin, showed an ID50 of 0.3 μmol/cm2 and prevented ear oedema more effectively than an equimolar dose of indomethacin within 24 h.