Publications by authors named "Li-feng Sima"
A series of N-substituted desloratadine analogues were designed and synthesized. They were tested for H1 antihistamine activity by inhibiting histamine-induced contraction of isolated ileum muscles of guinea-pigs in vitro and inhibiting histamine-induced asthmatic reaction in guinea-pigs in vivo. All the evaluated compounds exhibited significant antihistamine activity compared with desloratadine.
View Article and Find Full Text PDFArticle Synopsis
- * Most compounds showed strong antihistamine activity, with Compound 3, N-(3-hydroxy)propyl desloratadine, proving to be the most effective and having a better safety profile compared to desloratadine.
- * The research highlighted the importance of an oxygen atom in the side carbon chain for improving antihistamine activity.
Synthesis and antihistamine evaluations of novel loratadine analogues.
Bioorg Med Chem Lett
August 2011
A series of loratadine analogues containing hydroxyl group and chiral center were synthesized. The effect of the synthesized compounds on the histamine-induced contractions of guinea-pig ileum muscles was studied. In addition, the in vivo asthma-relieving effect of the analogues in the histamine induced asthmatic reaction in guinea-pigs was determined.
View Article and Find Full Text PDF