4878-14-2Relevant articles and documents
Discovery and optimization of (R)-prolinol-derived agonists of the Growth Hormone Secretagogue receptor (GHSR)
Zhai, Weixu,Flynn, Neil,Longhi, Daniel A.,Tino, Joseph A.,Murphy, Brian J.,Slusarchyk, Dorothy,Gordon, David A.,Pendri, Anna,Shi, Shuhao,Stoffel, Robert,Ma, Baoqing,Sofia, Michael J.,Gerritz, Samuel W.
supporting information; experimental part, p. 5083 - 5086 (2009/07/18)
The discovery and optimization of a novel series of prolinol-derived GHSR agonists is described. This series emerged from a 11,520-member solid-phase library targeting the GPCR protein superfamily, and the rapid optimization of low micromolar hits into single-digit nanomolar leads can be attributed to the solid-phase synthesis of matrix libraries, which revealed multiple non-additive structure-activity relationships. In addition, the separation of potent diastereomers highlighted the influence of the α-methyl stereochemistry of the phenoxyacetamide sidechain on GHSR activity.
Biological Evaluation of some New Nitrophenoxy/Halophenoxyaeetyl/Propionyl-2-mercaptobenzothiazoles
Khare,Srivastava,Mukharya
, p. 627 - 628 (2007/10/03)
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