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.
Current Medicinal Chemistry
Title: Diltiazem Analogues: The Last Ten Years on Structure Activity Relationships
Volume: 14 Issue: 3
Author(s): Roberta Budriesi, Barbara Cosimelli, Pierfranco Ioan, Emanuele Carosati, Maria P. Ugenti and Rraffaella Spisani
Affiliation:
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.
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Cite this article as:
Budriesi Roberta, Cosimelli Barbara, Ioan Pierfranco, Carosati Emanuele, Ugenti P. Maria and Spisani Rraffaella, Diltiazem Analogues: The Last Ten Years on Structure Activity Relationships, Current Medicinal Chemistry 2007; 14 (3) . https://dx.doi.org/10.2174/092986707779941122
DOI https://dx.doi.org/10.2174/092986707779941122 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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