37859-28-2Relevant academic research and scientific papers
Multifunctional iron-chelators with protective roles against neurodegenerative diseases
Nunes, Andreia,Marques, Sérgio M.,Quintanova, Catarina,Silva, Diana F.,Cardoso, Sandra M.,Chaves, Sílvia,Santos, M. Amélia
, p. 6058 - 6073 (2013/06/26)
The multifactorial nature of Alzheimer's disease (AD), and the absence of a disease modifying drug, makes the development of new multifunctional drugs an attractive therapeutic strategy. Taking into account the hallmarks of AD patient brains, such as low levels of acetylcholine, misfolding of proteins and associated beta-amyloid (Aβ) aggregation, oxidative stress and metal dyshomeostasis, we have developed a series of compounds that merge three different approaches: metal attenuation, anti-Aβ aggregation and anti-acetylcholinesterase activity. Therefore, 3-hydroxy-4-pyridinone (3,4-HP) and benzothiazole molecular moieties were selected as starting frameworks due to their well known affinity for iron and Aβ peptides, respectively. The linkers between these two main functional groups were selected on the basis of virtual screening, so that the final molecule could further inhibit the acetylcholinesterase, responsible for the cholinergic losses. We describe herein the design and synthesis of the new hybrid compounds, followed by the assessment of solution properties, namely iron chelation and anti-oxidant capacity. The compounds were bioassayed for their capacity to inhibit AChE, as well as self- and Zn mediated-Aβ1-42 aggregation. Finally, we assessed their effects on the viability of neuronal cells stressed with Aβ42.
Design, synthesis and neuroprotective evaluation of novel tacrine-benzothiazole hybrids as multi-targeted compounds against Alzheimer's disease
Keri, Rangappa S.,Quintanova, Catarina,Marques, Sérgio M.,Esteves, A. Raquel,Cardoso, Sandra M.,Santos, M. Amélia
, p. 4559 - 4569 (2013/07/26)
Alzheimer's disease (AD) is a multifactorial disorder with several target proteins contributing to its etiology. In search for multifunctional anti-AD drug candidates, taking into account that the acetylcholinesterase (AChE) and beta-amyloid (Aβ) aggregat
Synthesis and in vitro antimicrobial activity of novel 2-(4-(substituted- carboxamido)benzyl/phenyl)benzothiazoles
Yilmaz, Serap,Yalcin, Ismail,Kaynak-Onurdag, Fatma,Ozgen, Selda,Yildiz, Ilkay,Aki, Esin
, p. 223 - 231 (2013/11/06)
A new series of 2-[4-(4-substitutedbenzamido/phenylacetamido/ phenylpropionamido) benzyl/phenyl]benzothiazole derivatives (6a-6w) were synthesized and evaluated for antibacterial and antifungal activities against Staphylococcus aureus, Bacillus subtilis,
Benzazole compounds
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, (2008/06/13)
There are disclosed herein benzazole compounds, exemplified by 2-(4-aminophenyl)benzothiazole and analogues or salts thereof, which exhibit very significant selective cytotoxic activity in respect of tumor cells, especially breast cancer cells, and which provide potentially useful chemotherapeutic agents for treatment of breast cancer.
