72594-22-0Relevant academic research and scientific papers
Design and Identification of a Novel, Functionally Subtype Selective GABAA Positive Allosteric Modulator (PF-06372865)
Owen, Robert M.,Blakemore, David,Cao, Lishuang,Flanagan, Neil,Fish, Rebecca,Gibson, Karl R.,Gurrell, Rachel,Huh, Chan Woo,Kammonen, Juha,Mortimer-Cassen, Elisabeth,Nickolls, Sarah A.,Omoto, Kiyoyuki,Owen, Dafydd,Pike, Andy,Pryde, David C.,Reynolds, David S.,Roeloffs, Rosemarie,Rose, Colin,Stead, Clara,Takeuchi, Mifune,Warmus, Joseph S.,Watson, Christine
supporting information, p. 5773 - 5796 (2019/05/15)
The design, optimization, and evaluation of a series of novel imidazopyridazine-based subtype-selective positive allosteric modulators (PAMs) for the GABAA ligand-gated ion channel are described. From a set of initial hits multiple subseries were designed and evaluated based on binding affinity and functional activity. As designing in the desired level of functional selectivity proved difficult, a probability-based assessment was performed to focus the project's efforts on a single subseries that had the greatest odds of delivering the target profile. These efforts ultimately led to the identification of two precandidates from this subseries, which were advanced to preclinical safety studies and subsequently to the identification of the clinical candidate PF-06372865.
Synergy of anodic oxidation and cathodic reduction leads to electrochemical deoxygenative C2 arylation of quinoline: N-oxides
Yuan, Yong,Jiang, Minbao,Wang, Tao,Xiong, Yunkui,Li, Jun,Guo, Huijiao,Lei, Aiwen
supporting information, p. 11091 - 11094 (2019/09/20)
The first example of electrochemical deoxygenative C2 arylation of quinoline N-oxides using sulfonyl hydrazines was demonstrated in this work. By employing both anodic oxidation and cathodic reduction, a variety of 2-arylquinolines were synthesized under metal catalyst-, exogenous-oxidant-, and exogenous-reductant-free conditions.
Gold-Catalyzed Dehydrazinative C(sp)–S Coupling Reactions of Arylsulfonyl Hydrazides with Ethynylbenziodoxolones for Accessing Alkynyl Sulfones
Shinde, Popat S.,Patil, Nitin T.
, p. 3512 - 3515 (2017/07/04)
A gold(III)-catalyzed dehydrazinative coupling reaction between arylsulfonyl hydrazides and ethynylbenziodoxolone reagents was realized for the synthesis of alkynyl sulfones. The scope and versatility of the reaction were demonstrated by the efficient synthesis of 23 derivatives with diverse structural features.
