Halogenated derivatives of boldine with high selectivity for α1A-adrenoceptors in rat cerebral cortex

Antinociceptive and free radical scavenging activities of alkaloids isolated from Lindera angustifolia Chen

“…The biological activities and efficacy of these compounds depend on the structures of substituted groups and their position on the skeleton. The results of structure-activity relationship (SAR) studies on their adrenoceptor antagonist (Madrero et al, 1996;Martinez et al, 1999;Indra et al, 2002), cytotoxic (Likhitwitayawuid et al, 1993), antioxidative (Martinez et al, 1992;Cassels et al, 1995), antiplatelet aggregation (Chen et al, 1996(Chen et al, , 2000, immunosuppressant (Philipov et al, 1998) and antivirus activities (Boustie et al, 1998;Zhang et al, 2002) have been reported previously. Although a broad spectrum of bioactivities and SAR of the aporphine and benzylisoquinoline alkaloids have been reported, their antinociceptive effects have been rarely investigated.…”

Antioxidant and Toxicity Activity in Vitro of Twelve Safrole Derivatives

“…Such structural changes are directly related to free radical scavenging activity and the cytotoxic activity 12 . On the other hand, In vitro studies and experiments in animal models suggest that the pharmacological activities such as cytoprotective, antitumoral promoting, antiinflammatory, antipyretic and antiplatelet activities have been associated with the ability of fenolic compounds to scavenge highly reactive free radicals 13,14 . In this sense, there is evidence that synthetic antioxidants, some of which possess hydroxyl and nitro groups in their structures, inhibit LDL oxidation and cardioprotective effects [15][16][17][18] ; for this reason the antioxidant capacity of safrole derivatives with phenolic structure and nitro substituent's, might give us excellent a priori information about this property when not yet studied.…”

Aporphinoid Antagonists of 5‐HT2A Receptors: Further Evaluation of Ring A Substituents and the Size of Ring C

“…Ivorra et al . have studied the effect of C3 halogenation of boldine ( 20 ) on affinity for α 1 adrenergic receptor subtypes (i.e., α 1A , α 1B , and α 1D receptors) . Here, it was found that bromination or chlorination at C3 improved affinity and selectivity for α 1A receptors.…”