Titre du document / Document title
Diltiazem analogues : The last ten years on structure activity relationships
Auteur(s) / Author(s)
BUDRIESI Roberta (1) ;
COSIMELLI Barbara (2) ;
IOAN Pierfranco (1) ;
CAROSATI Emanuele (3) ;
UGENTI Maria P. (1) ;
SPISANI Rraffaella (4) ;
Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)
(1) Dipartimento di Scienze Farmaceutiche, Università degli Studi di Bologna, Via Belmeloro 6, 40126 Bologna, ITALIE
(2) Dipartimento di Chimica Farmaceutica e Tossicologica, Università degli Studi di Napoli "Federico II", Via Montesano 49, 80131 Napoli, ITALIE
(3) Dipartimento di Chimica, Università di Perugia, via Elce di Sotto 10, 06123 Perugia, ITALIE
(4) Dipartimento di Chimica Organica "A. Mangini", Università degli Studi di Bologna, Via S. Giacomo 11, 40126 Bologna, ITALIE
Résumé / Abstract
Cardiovascular diseases as hypertension, angina and/or supraventricular arrhythmias are among the most important death causes in the world. For the treatment of heart pathologies, calcium channel entry blockers are very important drugs, owing to their therapeutic versatility. Although few calcium antagonists described until today are structurally related to diltiazem and to the benzothiazepine class, the still high pharmaceutical interest on diltiazem analogues justifies this review. Diltiazem and its first analogues developed in the early '70s became popular in the '80s, and were pharmacologically characterized for a long time. It is in the '90s that several research groups carried out structural variations identifying novel scaffolds for diltiazem-related compounds, with significant calcium antagonist behaviour. Recently, a series of thiazino-oxadiazolone derivatives were identified as potent and selective antagonists for calcium influx into cardiac cells, and they were subsequently used to search for novel chemotypes by means of virtual screening techniques. The resulting hits could open interesting perspectives for the development of drugs to treat cardiovascular diseases. In the present review, an updated collection of diltiazem analogues is reported over the last ten years. The chemical structure and the structure activity relationships will be given, with additional mention to the potential therapeutic applications.
Revue / Journal Title
Current medicinal chemistry
ISSN
0929-8673
Source / Source
2007, vol. 14, n
o3, pp. 279-287 [9 page(s) (article)] (61 ref.)
Langue / Language
Anglais
Editeur / Publisher
Bentham, Oak Park, IL, ETATS-UNIS
(1994)
(Revue)
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Localisation / Location
INIST-CNRS, Cote INIST : 22999, 35400014557079.0040
Nº notice refdoc (ud4) : 18540286
