Indole Mannich bases and their antimycobacterial effect.
3-[(4-arylpiperazin-1-yl)methyl]lindoles (2a-h) and 3-[(4-hydroxy-4-phenylpiperazin-1-yl)methyl]indole (3) were prepared and characterized by 1H NMR and mass spectrometry. All eight compounds (2a-c, e-h and 3) tested inhibited in vitro the growth of Mycobacterium tuberculosis H37Rv in the range of 98-7% at a concentration of > or = 6.25 microg/ml. From the preliminary microbiological data it is possible to observe that a simple increasing of lipophilicity of the compounds tested to above logPcalc> or =3.8 significantly increases the potencies of their antitubercular action.
Malinka
Wiesław
W
Department of Chemistry of Drugs, Wrocław Medical University, Poland.
Swiatek
Piotr
P
D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology*; D008352:Mannich Bases / Q000737:chemistry / Q000494:pharmacology*; D009169:Mycobacterium tuberculosis / Q000187:drug effects / Q000254:growth & development
D000900:Anti-Bacterial Agents; D007211:Indoles; D008352:Mannich Bases