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Synthesis and antihistamine evaluations of novel loratadine analogues |
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| Authors: | Wang Yue Wang Juan Lin Yan Si-Ma Li-Feng Wang Dong-hua Chen Li-Gong Liu Deng-Ke |
| Institution: | a School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, PR China b School of Chemical Engineering, Shijiazhuang University, Shijiazhuang, Hebei 050035, PR China c School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, PR China d Tianjin Institute of Pharmaceutical Research, Tianjin 300072, PR China |
| Abstract: | 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. |
| Keywords: | Synthesis Antihistamine Loratadine |
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