title: Antimycobacterial and H1-antihistaminic activity of 2-substituted piperidine derivatives.
abstract: 2-Substituted derivatives of the antihistaminic agents Bamipine, Diphenylpyraline and of their 1-phenyl analogues were tested for their antimycobacterial and H(1)-antagonistic activities. They are strong H1-receptor antagonists and also inhibit the growth of mycobacterials with a maximum MIC of 6.25 microg/mL against Mycobacterium tuberculosis H(37)Rv. H1-receptor antagonistic potency was slightly decreased by substitution in ring position 2 and distinctly diminished by N-aryl substitution. The antimycobacterial potency of Diphenylpyraline was in general increased by substitution in ring position 2, whereas only a few Bamipine derivatives showed markedly improved activity. A correlation between the two activities was not detected for those compounds.
authors.affiliation: Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Universitätsplatz 1, A-8010 Graz, Austria. robert.weis@uni-graz.at
authors.forename: Robert
authors.initials: R
authors.lastname: Weis
authors.forename: Klaus
authors.initials: K
authors.lastname: Schweiger
authors.forename: Johanna
authors.initials: J
authors.lastname: Faist
authors.forename: Erich
authors.initials: E
authors.lastname: Rajkovic
authors.forename: Andreas J
authors.initials: AJ
authors.lastname: Kungl
authors.forename: Walter M F
authors.initials: WM
authors.lastname: Fabian
authors.forename: Walter
authors.initials: W
authors.lastname: Schunack
authors.forename: Werner
authors.initials: W
authors.lastname: Seebacher
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D002478:Cells, Cultured; D006168:Guinea Pigs; D006634:Histamine H1 Antagonists / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D006801:Humans; D008826:Microbial Sensitivity Tests; D010880:Piperidines / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity
chemical_list: D000900:Anti-Bacterial Agents; D006634:Histamine H1 Antagonists; D010880:Piperidines