AI Article Synopsis
- - The text discusses the development of spirocyclic piperidine-azetidine inverse agonists aimed at the ghrelin receptor, highlighting how issues with these compounds were identified and addressed.
- - A three-step synthesis process and a binding assay were employed to enhance the potency and ADMET (Adsorption, Distribution, Metabolism, Excretion, and Toxicity) characteristics of these compounds efficiently.
- - Compound 10 n, featuring a unique imidazo-thiazole acetamide and a phenyl triazole, demonstrates improved binding affinity and a lower logP value compared to the hit molecule 10a, indicating potential for further optimization in this compound series.
Article Abstract
The discovery of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor is described. The characterization and redressing of the issues associated with these compounds is detailed. An efficient three-step synthesis and a binding assay were relied upon as the primary means of rapidly improving potency and ADMET properties for this class of inverse agonist compounds. Compound 10 n bearing distributed polarity in the form of an imidazo-thiazole acetamide and a phenyl triazole is a unit lower in logP and has significantly improved binding affinity compared to the hit molecule 10a, providing support for further optimization of this series of compounds.
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| http://dx.doi.org/10.1016/j.bmcl.2012.05.024 | DOI Listing |
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