910300-34-4Relevant articles and documents
Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity
Tran, Joe A.,Tucci, Fabio C.,Jiang, Wanlong,Marinkovic, Dragan,Chen, Caroline W.,Arellano, Melissa,Markison, Stacy,Fleck, Beth A.,Wen, Jenny,White, Nicole S.,Pontillo, Joseph,Saunders, John,Marks, Daniel,Hoare, Sam R.,Madan, Ajay,Foster, Alan C.,Chen, Chen
, p. 5166 - 5176 (2008/03/13)
A series of pyrrolidinones derived from phenylalanines were synthesized as potent antagonists of the human melanocortin-4 receptor. These compounds showed high potencies and selectivities, and several of them had good oral bioavailabilities. In addition,
Arylpropionylpiperazines as antagonists of the human melanocortin-4 receptor
Jiang, Wanlong,Tucci, Fabio C.,Chen, Caroline W.,Arellano, Melissa,Tran, Joe A.,White, Nicole S.,Marinkovic, Dragan,Pontillo, Joseph,Fleck, Beth A.,Wen, Jenny,Saunders, John,Madan, Ajay,Foster, Alan C.,Chen, Chen
, p. 4674 - 4678 (2007/10/03)
A series of 3-arylpropionylpiperazines were synthesized as antagonists of the melanocortin-4 receptor. Their potency was found to be increased by replacing the α-methyl substituent of the initial lead 11 with a larger s-Bu or i-Bu group. Further potency enhancement was observed when a glycine or β-alanine was incorporated onto the benzylamine. Some compounds demonstrated good potency, moderate selectivity, and oral bioavailability.
