Design and synthesis of novel small molecule N/OFQ receptor antagonists.
Small molecule N/OFQ receptor antagonists were designed and synthesized to further investigate the therapeutic potential of N/OFQ receptor modulators. The resulting octahydrobenzimidazol-2-ones 14 and 23 show excellent antagonistic activity towards both N/OFQ and mu receptors with high affinity to the human N/OFQ receptor.
Drug Discovery, Purdue Pharma L.P., 6 Cedar Brook Drive, Cranbury, NJ 08512, USA. zhengming.chen@pharma.com
Zhengming
Z
Chen
R Richard
RR
Goehring
Kenneth J
KJ
Valenzano
Donald J
DJ
Kyle
D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D015195:Drug Design; D006801:Humans; D009292:Narcotic Antagonists; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011485:Protein Binding; D011957:Receptors, Opioid; D000094942:Nociceptin Receptor
D001562:Benzimidazoles; C402921:J 113397; D009292:Narcotic Antagonists; D010880:Piperidines; D011957:Receptors, Opioid; D000094942:Nociceptin Receptor; C000722283:OPRL1 protein, human