711010-35-4Relevant academic research and scientific papers
NPY-5 antagonists
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Page 17, (2008/06/13)
The present invention provides NPY-5 receptor antagonists having a Formula (I) Methods and pharmaceutical compositions useful for treating diseases, conditions and/or disorders modulated by the above NPY-5 receptor antagonists are also provided.
Structure-activity relationships in a series of NPY Y5 antagonists: 3-Amido-9-ethylcarbazoles, core-modified analogues and amide isosteres
Hammond, Marlys,Elliott, Richard L.,Gillaspy, Melissa L.,Hager, David C.,Hank, Richard F.,LaFlamme, Janet A.,Oliver, Robert M.,DaSilva-Jardine, Paul A.,Stevenson, Ralph W.,Mack, Christine M.,Cassella, James V.
, p. 1989 - 1992 (2007/10/03)
Beginning with carbazole 1a, the amide and alkyl substituents were optimized to maintain potency while adding solubilizing groups. Efforts to replace the 3-amino-9-ethylcarbazole core, a known carcinogen, used the SAR generated in the carbazole series for guidance and led to the synthesis of a number of core-modified analogues. In addition, an isosteric series, in which the amide was replaced with an imidazole, was prepared. Two potent new series lacking the putative toxicophore were identified from these endeavors.
