دورية أكاديمية

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

التفاصيل البيبلوغرافية
العنوان: Cardiovascular Profile of Xanthone-Based 1,4 Dihydropyridines Bearing a Lidoflazine Pharmacophore Fragment.
المؤلفون: Bisi A; Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via Belmeloro, 6, 40126 Bologna, Italy. alessandra.bisi@unibo.it., Micucci M; Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via Belmeloro, 6, 40126 Bologna, Italy. matteo.micucci2@unibo.it., Gobbi S; Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via Belmeloro, 6, 40126 Bologna, Italy. silvia.gobbi@unibo.it., Belluti F; Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via Belmeloro, 6, 40126 Bologna, Italy. federica.belluti@unibo.it., Budriesi R; Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via Belmeloro, 6, 40126 Bologna, Italy. roberta.budriesi@unibo.it., Rampa A; Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via Belmeloro, 6, 40126 Bologna, Italy. angela.rampa@unibo.it.
المصدر: Molecules (Basel, Switzerland) [Molecules] 2018 Nov 27; Vol. 23 (12). Date of Electronic Publication: 2018 Nov 27.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: MDPI Country of Publication: Switzerland NLM ID: 100964009 Publication Model: Electronic Cited Medium: Internet ISSN: 1420-3049 (Electronic) Linking ISSN: 14203049 NLM ISO Abbreviation: Molecules Subsets: MEDLINE
أسماء مطبوعة: Original Publication: Basel, Switzerland : MDPI, c1995-
مواضيع طبية MeSH: Dihydropyridines*/chemical synthesis , Dihydropyridines*/chemistry , Dihydropyridines*/pharmacology , Lidoflazine*/chemical synthesis , Lidoflazine*/chemistry , Lidoflazine*/pharmacology , Xanthones*/chemical synthesis , Xanthones*/chemistry , Xanthones*/pharmacology, Calcium Channels, L-Type/*metabolism , Myocardial Contraction/*drug effects , Myocardium/*metabolism, Animals ; Female ; Guinea Pigs ; Male
مستخلص: 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 ( 4a ⁻ e ), and thus a possible preferential binding with the Ca v 1.2 isoform of l-type calcium channels, which are mainly involved in cardiac contractility.
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فهرسة مساهمة: Keywords: 1,4-dihydropyridine; calcium channels; hybrid compounds; lidoflazine; xanthone
المشرفين على المادة: 0 (Calcium Channels, L-Type)
0 (Dihydropyridines)
0 (L-type calcium channel alpha(1C))
0 (Xanthones)
7M8K3P6I89 (1,4-dihydropyridine)
9749WEV0CA (xanthone)
J4ZHN3HBTE (Lidoflazine)
تواريخ الأحداث: Date Created: 20181130 Date Completed: 20190129 Latest Revision: 20200225
رمز التحديث: 20221213
مُعرف محوري في PubMed: PMC6321116
DOI: 10.3390/molecules23123088
PMID: 30486354
قاعدة البيانات: MEDLINE
الوصف
تدمد:1420-3049
DOI:10.3390/molecules23123088