Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy was written by Cameron, Kimberly O.;Kung, Daniel W.;Kalgutkar, Amit S.;Kurumbail, Ravi G.;Miller, Russell;Salatto, Christopher T.;Ward, Jessica;Withka, Jane M.;Bhattacharya, Samit K.;Boehm, Markus;Borzilleri, Kris A.;Brown, Janice A.;Calabrese, Matthew;Caspers, Nicole L.;Cokorinos, Emily;Conn, Edward L.;Dowling, Matthew S.;Edmonds, David J.;Eng, Heather;Fernando, Dilinie P.;Frisbie, Richard;Hepworth, David;Landro, James;Mao, Yuxia;Rajamohan, Francis;Reyes, Allan R.;Rose, Colin R.;Ryder, Tim;Shavnya, Andre;Smith, Aaron C.;Tu, Meihua;Wolford, Angela C.;Xiao, Jun. And the article was included in Journal of Medicinal Chemistry in 2016.Application In Synthesis of 6-Chloro-5-(4-(1-hydroxycyclobutyl)phenyl)-1H-indole-3-carboxylic acid This article mentions the following:
Adenosine monophosphate-activated protein kinase (AMPK) is a protein kinase involved in maintaining energy homeostasis within cells. On the basis of human genetic association data, AMPK activators were pursued for the treatment of diabetic nephropathy. Identification of an indazole amide high throughput screening (HTS) hit followed by truncation to its minimal pharmacophore provided an indazole acid lead compound Optimization of the core and aryl appendage improved oral absorption and culminated in the identification of indole acid, PF-06409577 (7). Compound 7 was advanced to first-in-human trials for the treatment of diabetic nephropathy. In the experiment, the researchers used many compounds, for example, 6-Chloro-5-(4-(1-hydroxycyclobutyl)phenyl)-1H-indole-3-carboxylic acid (cas: 1467057-23-3Application In Synthesis of 6-Chloro-5-(4-(1-hydroxycyclobutyl)phenyl)-1H-indole-3-carboxylic acid).
6-Chloro-5-(4-(1-hydroxycyclobutyl)phenyl)-1H-indole-3-carboxylic acid (cas: 1467057-23-3) belongs to indole derivatives. Indole, first isolated in 1866, and it is commonly synthesized from phenylhydrazine and pyruvic acid, although several other procedures have been discovered.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Application In Synthesis of 6-Chloro-5-(4-(1-hydroxycyclobutyl)phenyl)-1H-indole-3-carboxylic acid
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Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles