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Example sentences for: orjales

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Recent studies have expanded on this model to include another lipophilic region and a second hydrogen bonding interaction two atoms away from the first [ 19 20 21 ] . A compound that contains all five pharmacophoric regions was synthesized by Orjales et al [ 22 ] . This compound (1-(phenylmethyl)-2-piperizinyl benzimidazole or lerisetron) is shown in figure 1and is a potent 5-HT 3 R antagonist.
All target molecules were prepared according to a general 2-step synthesis reported previously by Orjales et al . with only slight modification [ 22 23 ] . Commercially available 2-chlorobenzimidazole, in dry DMF was treated with a slight excess of NaH, (1.
While Lerisetron contains no carbonyl group, the second nitrogen contained in the benzimidazole heterocycle could act as bioisostere of this functional group [ 22 ] . Orjales demonstrated the importance of the N-benzyl group by synthesizing several N1 substituted analogs of Lerisetron.