Literature DB >> 30861492

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

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.
Copyright © 2019 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  1,4-Dihydropyridines; Calcium channels blockers; Imidazo[2,1-b]thiazoles; Neuroprotection

Mesh:

Substances:

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


  4 in total

Review 1.  Role of the Platelets and Nitric Oxide Biotransformation in Ischemic Stroke: A Translative Review from Bench to Bedside.

Authors:  Maciej Bladowski; Jakub Gawrys; Damian Gajecki; Ewa Szahidewicz-Krupska; Anna Sawicz-Bladowska; Adrian Doroszko
Journal:  Oxid Med Cell Longev       Date:  2020-08-28       Impact factor: 6.543

2.  3-Aryl-4-nitrobenzothiochromans S,S-dioxide: From Calcium-Channel Modulators Properties to Multidrug-Resistance Reverting Activity.

Authors:  Matteo Micucci; Maurizio Viale; Alberto Chiarini; Domenico Spinelli; Maria Frosini; Cinzia Tavani; Massimo Maccagno; Lara Bianchi; Rosaria Gangemi; Roberta Budriesi
Journal:  Molecules       Date:  2020-02-27       Impact factor: 4.411

Review 3.  The Expanding Role of Pyridine and Dihydropyridine Scaffolds in Drug Design.

Authors:  Yong Ling; Zhi-You Hao; Dong Liang; Chun-Lei Zhang; Yan-Fei Liu; Yan Wang
Journal:  Drug Des Devel Ther       Date:  2021-10-13       Impact factor: 4.162

4.  Four-Component Fusion Protocol with NiO/ZrO2 as a Robust Recyclable Catalyst for Novel 1,4-Dihydropyridines.

Authors:  Sandeep V H S Bhaskaruni; Suresh Maddila; Werner E van Zyl; Sreekantha B Jonnalagadda
Journal:  ACS Omega       Date:  2019-12-05
  4 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.