1,721,042 research outputs found
3-Iodothyronamine and Derivatives: New Allies Against Metabolic Syndrome?
No full textIn the two decades since its discovery, a large body of evidence has amassed to highlight the potential of 3-iodothyronamine (T1AM) as an antiobesity drug, whose pleiotropic signaling actions profoundly impact energy metabolism. In the present review, we recapitulate the most relevant properties of T1AM, including its structural and functional relationship to thyroid hormone, its endogenous levels, molecular targets, as well as its genomic and non-genomic effects on metabolism elicited in experimental models after exogenous administration. The physiological and pathophysiological relevance of T1AM in the regulation of energy homeostasis and metabolism is also discussed, along with its potential therapeutic applications in metabolic disturbances. Finally, we examine a number of T1AM analogs that have been recently developed with the aim of designing novel pharmacological agents for the treatment of interlinked diseases, such as metabolic and neurodegenerative disorders, as well as additional synthetic tools that can be exploited to further explore T1AM-dependent mechanisms and the physiological roles of trace amine-associated receptor 1 (TAAR1)-mediated effects
H2S-BASED THERAPEUTIC AGENTS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
No full textThe present invention concerns the field of neurodegenerative diseases, and in particular relates to compounds, pharmaceutical compositions and their uses in the protection of neuronal cells from inflammation and from oxidative stress in the early stage of Parkinson's Disease as well as in Alzheimer's Disease
H2S-BASED THERAPEUTIC AGENTS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
No full textThe present invention concerns the field of neurodegenerative diseases, and in particular relates to compounds, pharmaceutical compositions and their uses in the protection of neuronal cells from inflammation and from oxidative stress in the early stage of Parkinson's Disease as well as in Alzheimer's Disease
2-OXO-1,2-DIHYDROPYRIDINE-3-CARBOXAMIDE COMPOUNDS AND THEIR USE AS INHIBITORS OF PDK1 (US Patent App. 15/735,468, 2018)
No full textThe present invention concern a 2-oxo-1,2-dihydropyridine-3-carboxamide compound of Formula (I) and new 2-oxo-1,2-dihydropyridine-3-carboxamide compounds of Formula (II) in the treatment of pathologies which require an inhibitor of PDK1 enzyme such as diabetes, neurodegenerative diseases such as Alzheimer's and Prion Diseases, and tumours such as breast, and pancreatic cancers and glioblastoma, particularly glioblastoma
2-OXO-1,2-DIHYDROPYRIDINE-3-CARBOXAMIDE COMPOUNDS AND THEIR USE AS INHIBITORS OF PDK1 (US Patent App. 15/735,468, 2018)
No full textThe present invention concern a 2-oxo-1,2-dihydropyridine-3-carboxamide compound of Formula (I) and new 2-oxo-1,2-dihydropyridine-3-carboxamide compounds of Formula (II) in the treatment of pathologies which require an inhibitor of PDK1 enzyme such as diabetes, neurodegenerative diseases such as Alzheimer's and Prion Diseases, and tumours such as breast, and pancreatic cancers and glioblastoma, particularly glioblastoma
COMPOSTI 2-OXO-1,2-DIIDROPIRIDIN-3-CARBOSSAMMIDE E LORO USO COME INIBITORI DUALI DI PDK1/AurA”
No full textThe invention concerns 2-oxo-1,2-dihydropyridine-3-carboxamide compounds and
10 their use as dual inhibitors and/or modulators of PDK1/AurA
Oxidative stress, mitochondrial abnormalities and proteins deposition: multitarget approaches in Alzheimer's disease
Full text linkAlzheimer diseases (AD) is a multifactorial pathology characterized by a complex etiology. The hallmarks of AD, such as Aβ deposits in senile plaque and neurofibrillary tangles (NFT), are strongly intertwined with reactive oxygen species (ROS)production and oxidative stress (OS),which are considered the common effectors of the cascade of degenerative events. An increasing body of evidence reveals that both mitochondrial abnormalities and metal accumulations synergistically act as major producers of ROS, thus contributing to neuronal toxicity. Consequently, the detrimental role of ROS production together with the neurodegenerative events involved in AD has been widely investigated as new potential therapeutic strategies. This review will concisely summarize the link between OS and the hallmarks of AD, emphasizing on their strong correlation with neurodegenerative events and elucidating the pivotal role of ROS in AD pathology. Furthermore, through this review, we will provide a short account of some of the efforts, challenges and opportunities in developing multitarget drugs by addressing ROS production, metal accumulation and protein depositions
COMPOSTI 2-OXO-1,2-DIIDROPIRIDIN-3-CARBOSSAMMIDE E LORO USO COME INIBITORI DUALI DI PDK1/AurA”
No full textThe invention concerns 2-oxo-1,2-dihydropyridine-3-carboxamide compounds and
10 their use as dual inhibitors and/or modulators of PDK1/AurA
COMPOSTI 2-OXO-1,2-DIIDROPIRIDIN-3-CARBOSSAMMIDE E LORO USO COME INIBITORI DI PDK1.
No full textThe invention concerns 2-oxo-1,2-dihydropyridine-3-carboxamide compounds
10 and their use as inhibitors and/or modulators of PDK1
Hydrogen sulfide: A worthwhile tool in the design of new multitarget drugs
Full text linkH2S is a gaseous molecule able to trigger a plethora of central physiological and pharmacological effects as antioxidant, pro- and anti-inflammatory, pro- and anti-nociceptive, neuromodulator, and cytoprotective. The polypharmacology of H2S depends on the wide variety of targets implicated, but, despite the efforts, the mechanisms of action that should clarify its activity are still not completely unrevealed. Nevertheless, many attempts to exploit the multifaceted profile of this molecule have already been accomplished and many chemical entities containing an H2S-releasing pharmacophore have been synthetized. Here we discuss recent investigations on multitarget molecules able to release H2S, with a particular focus on the combinations of "native drug" with moieties structurally able to release H2S and their applications as therapeutic tools in bone disease, gastrointestinal system and neurodegenerative disorders
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