POTENTIAL GABA(B) RECEPTOR ANTAGONISTS .8. THE SYNTHESIS OF 3-AMINO-N-ARYL-2-HYDROXY-PROPANE-1-SULFONAMIDES AND ANALOGS OF BACLOFEN CONTAINING NITRO-GROUPS

3-Amino-N-aryl-2-hydroxypropane-1-sulfonamides were synthesized by the reaction of the corresponding epoxy sulfonamide with sodium azide: fo llowed by reduction to the corresponding amine. The synthesis of 3-nit ropropan-1-amine and two 2-thienyl derivatives is also reported. o-2-h ydroxy-N-(4-nitrophenyl)propane-1-sulfonamide and 3-nitropropan-1-amin e were found to be specific antagonists of GABA at the GABAB receptor. Substitution of the amino group by alkyl or aryl groups reduced the a ctivity.