Identification and Optimization of Pyrrolidine Derivatives as Highly Potent Ghrelin Receptor Full Agonists was written by Cooper, Martin;Llinas, Antonio;Hansen, Peter;Caffrey, Moya;Ray, Asim;Sjoedin, Stina;Shamovsky, Igor;Wada, Hiroki;Jellesmark Jensen, Tina;Sivars, Ulf;Hultin, Leif;Andersson, Ulf;Lundqvist, Sara;Gedda, Karin;Jinton, Lisa;Krutroek, Nina;Lewis, Richard;Jansson, Paul;Gardelli, Cristina. And the article was included in Journal of Medicinal Chemistry in 2020.Formula: C10H6ClNO3 This article mentions the following:
Muscle atrophy and cachexia are common comorbidities among patients suffering from cancer, chronic obstructive pulmonary disease, and several other chronic diseases. The peptide hormone ghrelin exerts pleiotropic effects including the stimulation of growth hormone secretion and subsequent increase of insulin-like growth factor-1 levels, an important mediator of muscle growth and repair. Ghrelin also acts on inflammation, appetite, and adipogenesis and therefore has been considered a promising therapeutic target for catabolic conditions. We previously reported on the synthesis and properties of an indane based series of ghrelin receptor full agonists which led to a sustained increase of insulin-like growth factor-1 in a dog pharmacodynamic study. Herein we report on the identification of a series of pyrrolidine or piperidine based full agonists and attempted optimization to give compounds with profiles suitable for progression as clin. candidates. In the experiment, the researchers used many compounds, for example, 5-(2-Chlorophenyl)-3-isoxazolecarboxylic Acid (cas: 334017-34-4Formula: C10H6ClNO3).
5-(2-Chlorophenyl)-3-isoxazolecarboxylic Acid (cas: 334017-34-4) belongs to benzisoxazole derivatives. Many fluorinated compounds, 1,2-benzisoxazole derivatives and various amides are currently used in the treatment of diseases. The benzisoxazole template forms the molecular backbone, possesses versatile binding properties with a frequently occurring binding motif, and provides potent and selective ligands for a range of different biological targets in medicinal chemistry.Formula: C10H6ClNO3
Referemce:
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics