Author/Authors :
Lawrence A. Black، نويسنده , , Diana L. Nersesian، نويسنده , , Padam Sharma، نويسنده , , Yi-Yin Ku، نويسنده , , Youssef L. Bennani، نويسنده , , Kennan C. Marsh، نويسنده , , Thomas R. Miller، نويسنده , , Timothy A. Esbenshade، نويسنده , , Arthur A. Hancock، نويسنده , , Marlon Cowart، نويسنده ,
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-methylpyrrolidine substituent possessing the greatest rat and human H3 receptor binding affinities.
