4-[6-(2-Aminoethyl) naphthalen-2-yl] benzonitriles are potent histamine H 3 receptor antagonists with high CNS penetration

…, DL Nersesian, P Sharma, YY Ku, YL Bennani…

Index: Black, Lawrence A.; Nersesian, Diana L.; Sharma, Padam; Ku, Yi-Yin; Bennani, Youssef L.; Marsh, Kennan C.; Miller, Thomas R.; Esbenshade, Timothy A.; Hancock, Arthur A.; Cowart, Marlon Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 5 p. 1443 - 1446

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Citation Number: 20

Abstract

4-[6-(2-Tertiaryaminoethyl) naphthalen-2-yl] benzonitriles are conformationally constrained histamine H3 receptor antagonists with high potency and selectivity. The analogs were designed around a naphthalene core, with the goal of enhancing lipophilicity and CNS penetration, as compared to a previously reported benzofuran series. The SAR of the tertiary amine moiety is similar to that reported for the benzofuran series, with analogs bearing a 2 ...