Antimycobacterial and H1-antihistaminic activity of 2-substituted piperidine derivatives.

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Weis R, Schweiger K, Faist J, Rajkovic E, Kungl AJ, Fabian WM, Schunack W, Seebacher W

Antimycobacterial and H1-antihistaminic activity of 2-substituted piperidine derivatives.

Bioorg Med Chem. 2008 Dec 15;16(24):10326-31. doi: 10.1016/j.bmc.2008.10.042. Epub 2008 Oct 22.

PubMed ID

18977145 [ View in PubMed

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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.

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Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Diphenylpyraline	Histamine H1 receptor	Protein	Humans	Yes	Antagonist	Details