Antimycobacterial and H1-antihistaminic activity of 2-substituted piperidine derivatives |
| |
Authors: | Weis Robert Schweiger Klaus Faist Johanna Rajkovic Erich Kungl Andreas J Fabian Walter M F Schunack Walter Seebacher Werner |
| |
Institution: | Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Universit?tsplatz 1, A-8010 Graz, Austria. robert.weis@uni-graz.at |
| |
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. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|