Rapid parallel synthesis applied to the optimization of a series of potent nonpeptide neuropeptide Y-1 receptor antagonists
…, MP Clay, DA Schober, AM Van Abbema, DW Johnson…
Index: Siegel, Miles G.; Chaney, Michael O.; Bruns, Robert F.; Clay, Michael P.; Schober, Douglas A.; Van Abbema, Anne M.; Johnson, Douglas W.; Cantrell, Buddy E.; Hahn, Patric J.; Hunden, David C.; Gehlert, Donald R.; Zarrinmayeh, Hamideh; Ornstein, Paul L.; Zimmerman, Dennis M.; Koppel, Gary A. Tetrahedron, 1999 , vol. 55, # 39 p. 11619 - 11639
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Citation Number: 18
Abstract
This study describes the integrated application of parallel synthesis and computational chemistry to the design of potent nonpeptide antagonists for the neuropeptide Y-1 (NPY1) receptor. A lead molecule was modeled in the active site of the NPY1 receptor, and a potentially fruitful region for analog construction was identified. Synthesis of suitable scaffolds followed by solution phase generation of a small library of analogs produced a ...