10330-59-3Relevant academic research and scientific papers
Synthesis, Structure-Activity Relationships, and Preclinical Evaluation of Heteroaromatic Amides and 1,3,4-Oxadiazole Derivatives as 5-HT4 Receptor Partial Agonists
Nirogi, Ramakrishna,Mohammed, Abdul Rasheed,Shinde, Anil K.,Gagginapally, Shankar Reddy,Kancharla, Durga Malleshwari,Middekadi, Vanaja Reddy,Bogaraju, Narsimha,Ravella, Srinivasa Rao,Singh, Pooja,Birangal, Sumit Raosaheb,Subramanian, Ramkumar,Palacharla, Raghava Choudary,Benade, Vijay,Muddana, Nageswararao,Jayarajan, Pradeep
, p. 4993 - 5008 (2018/05/29)
Alzheimer's disease (AD) is a neurodegenerative disorder that has a higher prevalence and incidence in people older than 60 years. The need for improved AD therapies is unmet as the current therapies are symptomatic with modest efficacy. Partial agonists of the 5-HT4 receptor (5-HT4R) offer both symptomatic and disease-modifying treatments as they shift amyloid-precursor-protein (APP) processing from the amyloidogenic pathway to the nonamyloidogenic pathway by activating the α-secretase enzyme. In addition, they also offer symptomatic treatment by increasing levels of the neurotransmitter acetylcholine in the brain. Because of this fascinating dual mechanism of action, several chemical scaffolds having 5-HT4R pharmacophores were designed and evaluated. Most of the synthesized compounds showed potent in vitro affinities and in vivo efficacies. Upon analysis of focused structure-activity relationships, compound 4o was identified as a potent 5-HT4R partial agonist with favorable ADME properties and good in vivo efficacy. GR-125487, a selective 5-HT4R antagonist, attenuated the activity of compound 4o in the novel-object-recognition-test cognition model.
Synthesis of functionalised 4H-quinolizin-4-ones via tandem Horner-Wadsworth-Emmons olefination/cyclisation
Muir, Calum W.,Kennedy, Alan R.,Redmond, Joanna M.,Watson, Allan J. B.
supporting information, p. 3337 - 3340 (2013/06/05)
4H-Quinolizin-4-ones are a unique class of heterocycle with valuable physicochemical properties and which are emerging as key pharmacophores for a range of biological targets. A tandem Horner-Wadsworth-Emmons olefination/cyclisation method has been developed to allow facile access to substituted 4H-quinolizin-4-ones encoded with a range of functional groups.
2-Pyridinyl β-ketones as new ligands for roomerature CuI-catalysed C-N coupling reactions
Wang, Deping,Ding, Ke
supporting information; experimental part, p. 1891 - 1893 (2009/10/23)
2-Pyridinyl β-ketones were identified as new efficient ligands for CuI-catalysed N-arylation of aliphatic amines at room temperature with great selectivity and substrate scope tolerance.
Two rare alkaloids from Pratia nummularia
Ho,Ou,Sun,Sun
, p. 567 - 568 (2007/10/03)
Two rare alkaloids, 1-(2-N-methylpiperidyl)-butan-2-one (1) and 1-(2-N-methylpiperidyl)-pentan-2-one (2), were identified from the medicinal plant Pratia nummularia. The structure of 1 was elucidated by means of spectroscopic methods. Compound 2 was established by spectral comparison with synthetic material.
