- Design, synthesis, and pharmacological characterization of 4-[4,4-Dimethyl-3-(4-hydroxybutyl)-5-oxo-2-thioxo-1-imidazolidinyl]-2-iodoben zonitrile as a high-affinity nonsteroidal androgen receptor ligand
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4-[4,4-Dimethyl-3-(4-hydroxybutyl)-5-oxo-2-thioxo-1-imidazolidinyl]-2-trifluo romethylbenzonitrile (RU 59063) is a prototype of a new class of high-affinity nonsteroidal androgen receptor (AR) ligands. The search for a radioiodinated AR ligand prompted us
- Van Dort,Robins,Wayburn
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Read Online
- NPY-5 antagonists
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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.
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- Synthesis of novel iodo derived bicalutamide analogs
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A series of optically active nonsteroidal selective androgen receptor modulators with structures analogous to bicalutamide was prepared by replacing the trifluoromethyl group with iodine and the sulfonyl linker by oxygen.
- Nair, Vipin A.,Mustafa, Suni M.,Mohler, Michael L.,Fisher, Scott J.,Dalton, James T.,Miller, Duane D.
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p. 9475 - 9477
(2007/10/03)
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- Structure-activity relationships in a series of NPY Y5 antagonists: 3-Amido-9-ethylcarbazoles, core-modified analogues and amide isosteres
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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.
- 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.
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p. 1989 - 1992
(2007/10/03)
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