Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 26, Issue 13, Pages 3773-3784Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2018.04.038
Keywords
Xanthone; Synthesis; Cardiovascular; Adrenoceptor; Hypertension; Arrhythmia
Funding
- Ministry of Science and Higher Education Poland [K/DSC/004307, K/ZDS/005487, K/ZDS/006235]
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A series of aminoisopropanoloxy derivatives of xanthone has been synthesized and their pharmacological properties regarding the cardiovascular system has been evaluated. Radioligand binding and functional studies in isolated organs revealed that title compounds present high affinity and antagonistic potency for alpha(1)-(compound 2 and 8), beta-(compounds 1, 3, 4, 7), alpha(1)/beta-(compounds 5 and 6) adrenoceptors. Furthermore, compound 7, the structural analogue of verapamil, possesses calcium entry blocking activity. The title compounds showed hypotensive and antiarrhythmic properties due to their adrenoceptor blocking effect. Moreover, they did not affect QRS and QT intervals, and they did not have proarrhythmic potential at tested doses. In addition they exerted anti-aggregation effect. The results of this study suggest that new compounds with multidirectional activity in cardiovascular system might be found in the group of xanthone derivatives. (C) 2018 Published by Elsevier Ltd.
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