| Literature DB >> 30861492 |
Alberto Leoni1, Maria Frosini2, Alessandra Locatelli1, Matteo Micucci1, Claudio Carotenuto2, Miriam Durante2, Sandro Cosconati3, Roberta Budriesi4.
Abstract
In the present work we describe the synthesis, characterization and evaluation of neuroprotective effects of a focused library of 4-imidazo[2,1-b]thiazole-1,4-dihydropyridines. Furthermore, the new dihydropyridines were subjected to functional in vitro assays in cardiac tissues and vascular smooth muscle to determine their possible selectivity in counteracting the effects of neurodegeneration. In particular the strategy adopted for designing the compounds involves the imidazo[2,1-b]thiazole nucleus. The observed properties show that substituents at C2 and C6 of the bicyclic scaffold are able to influence the cardiovascular parameters and the neuroprotective activity. In comparison to nifedipine, a set of derivatives such as compound 6, showed a neuroprotective profile of particular interest.Entities:
Keywords: 1,4-Dihydropyridines; Calcium channels blockers; Imidazo[2,1-b]thiazoles; Neuroprotection
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Year: 2019 PMID: 30861492 DOI: 10.1016/j.ejmech.2019.02.075
Source DB: PubMed Journal: Eur J Med Chem ISSN: 0223-5234 Impact factor: 6.514