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Influence of Hydroxyl Functional Group on the Structure and Stability of Xanthone: A Computational Approach
Open AccessFeature PaperArticle

Cardiovascular Profile of Xanthone-Based 1,4 Dihydropyridines Bearing a Lidoflazine Pharmacophore Fragment

Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via Belmeloro, 6, 40126 Bologna, Italy
Author to whom correspondence should be addressed.
Academic Editors: Maria Emília de Sousa, Honorina Cidade and Carlos Manuel Afonso
Molecules 2018, 23(12), 3088;
Received: 30 October 2018 / Revised: 21 November 2018 / Accepted: 23 November 2018 / Published: 27 November 2018
As a follow-up to our previous studies on differently substituted 1,4-dihydropyridines endowed with a peculiar cardiac selectivity, in this paper, a small series of hybrid compounds bearing the pharmacophore fragment of lidoflazine in position 2 or 3 on a 4-(xanthen-9-one)-dihydropyridine core was reported. Lidoflazine was selected due to our promising previously reported data, and the xanthen-9-one substituent was introduced in position 4 of the dihydropyridine scaffold based on the cardiac selectivity observed in several of our studies. The new hybrid compounds were tested to assess cardiac and vascular activities, and the data were evaluated in comparison with those previously obtained for 4-(xanthen-9-one)-dihydropyridines and lidoflazine–nifedipine hybrid compounds. The functional studies indicated an interesting peculiar selectivity for the cardiac parameter inotropy, in particular when the lidoflazine fragment was introduced in position 2 of the dihydropyridine scaffold (4ae), and thus a possible preferential binding with the Cav 1.2 isoform of l-type calcium channels, which are mainly involved in cardiac contractility. View Full-Text
Keywords: xanthone; 1,4-dihydropyridine; lidoflazine; calcium channels; hybrid compounds xanthone; 1,4-dihydropyridine; lidoflazine; calcium channels; hybrid compounds
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MDPI and ACS Style

Bisi, A.; Micucci, M.; Gobbi, S.; Belluti, F.; Budriesi, R.; Rampa, A. Cardiovascular Profile of Xanthone-Based 1,4 Dihydropyridines Bearing a Lidoflazine Pharmacophore Fragment. Molecules 2018, 23, 3088.

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