58088-72-5Relevant academic research and scientific papers
Asymmetric Transfer Hydrogenation of Densely Functionalized Diheteroaryl and Diaryl Ketones by a Ru-Catalyst of Minimal Stereogenicity
He, Dongxu,Xu, Xingjun,Lu, Yi,Zhou, Min-Jie,Xing, Xiangyou
, p. 8458 - 8463 (2020)
A highly enantioselective asymmetric transfer hydrogenation (ATH) of densely functionalized diheteroaryl and diaryl ketones was developed using Ru-catalysts of minimal stereogenicity. Various ketone substrates with structurally and electronically similar groups attached to the prochiral centers were reduced successfully in good to excellent enantioselectivities and yields. This protocol provides practical and efficient access to chiral diheteroarylmethanols and benzhydrols, which are key intermediates in pharmaceuticals and biologically active compounds.
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.
DOPAMINE D2 RECEPTOR LIGANDS
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Page/Page column 115; 117; 125; 126; 127; 128, (2016/07/05)
The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity.
