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Paper | Regular issue | Vol 24, No. 10, 1986, pp.2845-2855
Published online, 1st January, 1970
DOI: 10.3987/R-1986-10-2845
Synthesis of 3,6-Disubstituted β-Carbolines Which Possess either Benzodiazepine Antagonist or Agonist Activity

Timothy J. Hagen, Filadelfo Guzman, Christopher Schultz, James M. Cook,* Phil Skolnick, and Harlan E. Shannon

*Department of Chemistry, University of Wisconsin-Milwaukee, Milwaukee, Wisconsin 53201, U.S.A.

Abstract

A series of 3-substituted and 3,6-disubstituted β-carbolines have been synthesized. These compounds have been screened in vitro in order to determine the size of substituents which benzodiazepine receptors will tolerate at positions -3 and -6 of the β-carboline nucleus. It has been found that the receptor will tolerate ester alkyl groups at position-3 as large as cyclohexyl 1g but not as large as adamantyl 5d. Moreover, N-aryl substituents as large as naphthobenzylamino 8b can be introduced at position-6 without significant loss of receptor binding affinity.