Antimycobacterial and H1-antihistaminic activity of 2-substituted piperidine derivatives.
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.
Weis
Robert
R
Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Universitätsplatz 1, A-8010 Graz, Austria. robert.weis@uni-graz.at
Schweiger
Klaus
K
Faist
Johanna
J
Rajkovic
Erich
E
Kungl
Andreas J
AJ
Fabian
Walter M F
WM
Schunack
Walter
W
Seebacher
Werner
W
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
D000900:Anti-Bacterial Agents; D006634:Histamine H1 Antagonists; D010880:Piperidines