HETEROCYCLES, cilt.51, sa.11, ss.2561-2573, 1999 (SCI-Expanded)
A number of benzimidazoles, having several substituents on the azole and benzene nuclei and C-2 (methylamino, ethylenediamine, morpholine, piperazine and piperidine) were prepared. Regioselective synthesis was designed for the N-1-alkyl substituted benzimidazoles (14-15). X-Ray structure analysis of (14) was also revealed. Compounds were evaluated for their in vitro H-1-antihistaminic activity in the isolated guinea-pig ileum method. The compound (11) exhibits best activity.