New antihistaminic N-heterocyclic 4-piperidinamines. 1. Synthesis and antihistaminic activity of N-(4-piperidinyl)-1H-benzimidazol-2-amines

…, J Torremans, M Janssen, RA Stokbroekx…

Index: Janssens; Torremans; Janssen; Stokbroekx; Luyckx Journal of Medicinal Chemistry, 1985 , vol. 28, # 12 p. 1925 - 1933

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Citation Number: 71

Abstract

The synthesis of a series N-(4-piperidinyl)-lH-benzimidazol-2-amines and the preliminary evaluation of their in vitro and in vivo antihistaminic activity are described. Cyclodesulfurization of (2-aminopheny1) thioureas with mercury (I1) oxide resulted in 2- aminobenzimidazole intermediates, which were monoalkylated on the endo-nitrogen atom. After deprotection of the piperidine nitrogen atom with 48% aqueous hydrobromic acid ...