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

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

Bioorg Med Chem

Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Universitätsplatz 1, A-8010 Graz, Austria.

Published: December 2008

AI Article Synopsis

Article 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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Source
http://dx.doi.org/10.1016/j.bmc.2008.10.042DOI Listing

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