The discovery and structure-activity relationships of 2-(piperidin-3-yl)-1H-benzimidazoles as selective, CNS penetrating H1-antihistamines for insomnia

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 9, 2010, Pages 2916-2919

  Lavrador Erb, Karine ^a   Ravula, Satheesh Babu ^a   Yu, Jinghua ^a   Zamani Kord, Said ^a   Moree, Wilna J ^a   Petroski, Robert E ^a   Wen, Jianyun ^a   Malany, Siobhan ^a   Hoare, Samuel R J ^a   Madan, Ajay ^a   Crowe, Paul D ^a   Beaton, Graham ^a  

^a NEUROCRINE BIOSCIENCES INC   (United States)

Author keywords

Benzimidazole; CNS; H1 Antagonist; H1 Antihistamines; Insomnia, hERG; SAR; Sedative; Selective

Indexed keywords

2 (3 AMINOPIPERIDINE) BENZIMIDAZOLE DERIVATIVE; 2 (PIPERIDIN 3 YL) 1H BENZIMIDAZOLE DERIVATIVE; ANTIHISTAMINIC AGENT; BENZIMIDAZOLE; CYTOCHROME P450 3A4; NON PRESCRIPTION DRUG; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BLOOD BRAIN BARRIER; BLURRED VISION; CENTRAL NERVOUS SYSTEM; CONSTIPATION; CONTROLLED STUDY; DRUG ACTIVITY; DRUG HALF LIFE; DRUG PENETRATION; ENZYME INHIBITION; HUMAN; HUMAN TISSUE; IC 50; INSOMNIA; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION; TACHYCARDIA; URINE RETENTION; XEROSTOMIA;

BENZIMIDAZOLES; CENTRAL NERVOUS SYSTEM; DRUG DISCOVERY; ETHER-A-GO-GO POTASSIUM CHANNELS; HISTAMINE H1 ANTAGONISTS; HUMANS; SLEEP INITIATION AND MAINTENANCE DISORDERS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 77950864599     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.03.027     Document Type: Article

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