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.

Leoni, A., Frosini, M., Locatelli, A., Micucci, M., Carotenuto, C., Durante, M., et al. (2019). 4-Imidazo[2,1-b]thiazole-1,4-DHPs and neuroprotection: preliminary study in hits searching. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 169, 89-102 [10.1016/j.ejmech.2019.02.075].

4-Imidazo[2,1-b]thiazole-1,4-DHPs and neuroprotection: preliminary study in hits searching

Frosini M.;Carotenuto C.;
2019-01-01

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.
Leoni, A., Frosini, M., Locatelli, A., Micucci, M., Carotenuto, C., Durante, M., et al. (2019). 4-Imidazo[2,1-b]thiazole-1,4-DHPs and neuroprotection: preliminary study in hits searching. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 169, 89-102 [10.1016/j.ejmech.2019.02.075].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11365/1113646