1239701-58-6Relevant articles and documents
Synthesis and antihistamine evaluations of novel loratadine analogues
Wang, Yue,Wang, Juan,Lin, Yan,Si-Ma, Li-Feng,Wang, Dong-Hua,Chen, Li-Gong,Liu, Deng-Ke
, p. 4454 - 4456 (2011/09/15)
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. Most of the compounds exhibited definite H1 antihistamine activity. The S-enantiomers, compounds 2, 4 and 8, are more potent than the R-enantiomers, compounds 1, 3 and 7. Compound 6 was the most active one among the eight synthesized compounds.