Discovery and SAR development of 2-(phenylamino) imidazolines as prostacyclin receptor antagonists [corrected |
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Authors: | Clark Robin D Jahangir Alam Severance Daniel Salazar Rick Chang Thomas Chang David Jett Mary Frances Smith Steven Bley Keith |
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Institution: | Department of Medicinal Chemistry, Roche Palo Alto, 3431 Hillview Avenue, Palo Alto, CA 94304, USA. robin.clark5@verizon.net |
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Abstract: | On the basis of screening hits (1a,b), a series of selective, high affinity prostacyclin receptor antagonists was developed. The optimized lead compound 25d (4,5-dihydro-1H-imidazol-2-yl)-4-(4-isopropoxybenzyl)phenyl]amine] had analgesic activity in the rat. |
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