title: Synthesis and antihistamine evaluations of novel loratadine analogues.
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 H(1) 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.
authors: School of Chemical Engineering and Technology, Tianjin University, Tianjin, PR China.
authors: Yue
authors: Y
authors: Wang
authors: Juan
authors: J
authors: Wang
authors: Yan
authors: Y
authors: Lin
authors: Li-Feng
authors: LF
authors: Si-Ma
authors: Dong-hua
authors: DH
authors: Wang
authors: Li-Gong
authors: LG
authors: Chen
authors: Deng-Ke
authors: DK
authors: Liu
mesh_terms: D000818:Animals; D018926:Anti-Allergic Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D001249:Asthma / Q000188:drug therapy; D006168:Guinea Pigs; D006632:Histamine / Q000737:chemistry* / Q000378:metabolism; D006633:Histamine Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D007082:Ileum / Q000187:drug effects; D017336:Loratadine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use; D013237:Stereoisomerism
chemical_list: D018926:Anti-Allergic Agents; D006633:Histamine Antagonists; D017336:Loratadine; D006632:Histamine