Design and parallel synthesis of piperidine libraries targeting the nociceptin (N/OFQ) receptor.
Based on literature structures, we proposed a pharmacophore for NOP receptor ligands and used it as a guide for the design of a focused piperidine library and an optimization library. Potent NOP receptor agonists and antagonists were obtained from these libraries as well as a few potent, mu selective agonists.
Chen
Zhengming
Z
Computational, Combinatorial and Medicinal Chemistry, Purdue Pharma L.P., 6 Cedar Brook Drive, Cranbury, NJ 08512, USA. zhengming.chen@pharma.com
Miller
Wendy S
WS
Shan
Shen
S
Valenzano
Kenneth J
KJ
D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D015195:Drug Design; D009292:Narcotic Antagonists; D010880:Piperidines / Q000138:chemical synthesis*; D011957:Receptors, Opioid / Q000819:agonists*; D000094942:Nociceptin Receptor
D009292:Narcotic Antagonists; D010880:Piperidines; D011957:Receptors, Opioid; D000094942:Nociceptin Receptor