33098-11-2Relevant academic research and scientific papers
Optical molecular imaging of lysyl oxidase activity - detection of active fibrogenesis in human lung tissue
Aslam, Tashfeen,Miele, Amy,Chankeshwara, Sunay V.,Megia-Fernandez, Alicia,Michels, Chesney,Akram, Ahsan R.,McDonald, Neil,Hirani, Nik,Haslett, Chris,Bradley, Mark,Dhaliwal, Kevin
, p. 4946 - 4953 (2015)
Aberrant fibrogenesis is a feature of many diseases in multiple organ systems. The lysyl oxidase family of enzymes are central to tissue homeostasis and elevated lysyl oxidase activity is implicated in fibroproliferation as well as in cancer stroma. We have synthesised a novel fluorogenic reporter for monitoring lysyl oxidase activity that generates a 3-5 fold increase in fluorescence following probe activation in ventilating fibrotic ex vivo asinine lung and ex vivo human lung tissue. The probe termed "oLOX" can provide real-time measurement of lysyl oxidase activity in a number of biological settings and is tractable from an in vitro setting to man.
Design, synthesis and SAR analysis of novel potent and selective small molecule antagonists of NPBWR1 (GPR7)
Urbano, Mariangela,Guerrero, Miguel,Zhao, Jian,Velaparthi, Subash,Roberts, Edward,Adrian Saldanha, S.,Chase, Peter,Hodder, Peter,Wang, Zhiwei,Civelli, Olivier,Schaeffer, Marie-Therese,Brown, Steven,Rosen, Hugh
, p. 7135 - 7141,7 (2012/12/12)
Novel small molecule antagonists of NPBWR1 (GPR7) are herein reported. A high-throughput screening (HTS) of the Molecular Libraries-Small Molecule Repository library identified 5-chloro-4-(4-methoxyphenoxy)-2-(p-tolyl) pyridazin-3(2H)-one as a NPBWR1 hit antagonist with micromolar activity. Design, synthesis and structure-activity relationships study of the HTS-derived hit led to the identification of 5-chloro-2-(3,5-dimethylphenyl)-4-(4-methoxyphenoxy) pyridazin-3(2H)-one lead molecule with submicromolar antagonist activity at the target receptor and high selectivity against a panel of therapeutically relevant off-target proteins. This lead molecule may provide a pharmacological tool to clarify the molecular basis of the in vivo physiological function and therapeutic utility of NPBWR1 in diverse disease areas including inflammatory pain and eating disorders.
Efficient N-arylation of pyridazin-3(2H)-ones
Kim, Jeum-Jong,Park, Yong-Dae,Cho, Su-Dong,Kim, Ho-Kyun,Chung, Hyun A.,Lee, Sang-Gyeong,Falck,Yoon, Yong-Jin
, p. 8781 - 8784 (2007/10/03)
A variety of substituted pyridazin-3(2H)-ones are directly N-arylated in good yield using lead tetraacetate/zinc chloride in benzene or in substituted benzenes including chloro- and bromobenzene. A variety of substituted pyridazin-3(2H)-ones are directly N-arylated in good yield using lead tetraacetate/zinc chloride in benzene or in substituted benzenes including chloro- and bromobenzene.
