Identification of novel benzimidazole series of potent and selective ORL1 antagonists

A structurally novel ORL1 selective antagonist with a (piperazin-1-yl)benzimidazole scaffold was identified. Among them, an analogue 28 exhibited sub-nanomolar antagonistic activity. Structure–activity studies on benzimidazole lead 1 obtained from library screening led to the discovery of potent and...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2008-06, Vol.18 (11), p.3278-3281
Hauptverfasser:	Okamoto, Osamu, Kobayashi, Kensuke, Kawamoto, Hiroshi, Ito, Satoru, Satoh, Atsushi, Kato, Tetsuya, Yamamoto, Izumi, Mizutani, Sayaka, Hashimoto, Masaya, Shimizu, Atsushi, Sakoh, Hiroki, Nagatomi, Yasushi, Iwasawa, Yoshikazu, Takahashi, Hiroyuki, Ishii, Yasuyuki, Ozaki, Satoshi, Ohta, Hisashi
Format:	Artikel
Sprache:	eng
Schlagworte:	Benzimidazoles - chemical synthesis Benzimidazoles - chemistry Benzimidazoles - pharmacology Biological and medical sciences Combinatorial Chemistry Techniques Humans Medical sciences Molecular Structure Narcotic Antagonists Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Nociceptin receptor (NOP) Nociceptin/orphanin FQ Opioid receptor-like 1 (ORL1) antagonist Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Receptors, Opioid Structure-Activity Relationship
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