TABLE 1.

In vitro antifungal activities of acetylenic acids 1 to 7a

Species and strain or isolateIC50/MIC/MFC (μM) for compound no.b:
1234567
C. albicans
    ATCC 1405381.8/−/−>187.7c/−/−1.0/2.8/5.60.8/1.3/2.7>162.1/−/−−/−/−8.1/63.3/−
    ATCC 6019385.9/−/−150.0/−/−3.0/5.6/−1.6/2.7/−81.0/−/−−/−/−4.5/63.3/−
    ATCC 3235450.3/198.1/−187.7/−/−4.0/27.9/−1.6/8.0/−>162.1/−/−−/−/−4.0/31.7/−
    ATCC 9002856.8/99.1/−95.4/−/−2.0/2.8/11.11.3/2.7/−67.3/−/−−/−/−5.0/42.2/−
    ATCC 20095547.8/198.1/−66.7/−/−1.9/11.1/−0.9/1.3/−53.4/−/−−/−/−2.0/5.3/21.1
    Isolate 1d40.5/99.1/−82.2/−/−4.2/13.9/−1.7/2.7/−86.6/−/−−/−/−1.7/42.2/−
    Isolate 17d23.3/99.1/198.118.8/70.4/−3.6/16.7/−1.5/8.0/−55.0/−/−−/−/−3.5/42.2/−
Other Candida spp.
    C. glabrata ATCC 90030>198.1/−/−>187.7/−/−−/−/−−/−/−−/−/−−/−/−−/−/−
    C. krusei ATCC 62582.9/6.2/49.51.9/4.4/−3.4/5.6/−4.1/10.6/−106.1/−/−>178.7/−/−>168.9/−/−
    C. parapsilosis ATCC 22019>198.1/−/−−/−/−−/−/−−/−/−−/−/−−/−/−5.4/63.3/−
    C. tropicalis ATCC 75029.5/74.3/99.149.1/−/−6.3/111.4/−5.2/−/−−/−/−−/−/−27.7/−/−
C. neoformans e
    ATCC 9011352.4/−/−>187.7/−/−−/−/−−/−/−−/−/−−/−/−>168.9/−/−
    ATCC 660311.2/49.5/99.11.2/187.7/−1.4/−/−1.1/−/−−/−/−>178.6/−/−−/−/−
Aspergillus spp.
    A. fumigatus ATCC 2043059.4/37.1/198.136.6/140.8/−18.7/178.3/−1.1/2.7/−32.3/−/−−/−/−10.0/84.5/−
    A. fumigatus ATCC 90906165.6/−/−−/−/−−/−/−1.4/6.6/−81.0/−/−−/−/−13.3/84.5/−
    A. flavus ATCC 204304105.9/198.1/198.1−/−/−−/−/−−/−/−−/−/−−/−/−>168.9/−/−
    A. niger ATCC 16404100.9/−/−>187.7/−/−−/−/−−/−/−−/−/−−/−/−100.0/−/−
Trichophyton spp.
    T. mentagrophytes ATCC MYA-44393.9/9.3/12.43.0/5.9/5.91.2/2.8/2.80.4/0.7/0.7>162.1/−/−>178.6/−/−6.7/31.7/−
    T. mentagrophytes ATCC 95332.3/4.6/6.23.7/7.3/11.71.3/2.1/2.80.9/2.0/2.7−/−/−−/−/−14.2/21.1/−
    T. rubrum ATCC MYA-44383.8/31.0/198.14.1/29.3/−1.8/5.6/−0.6/3.3/−−/−/−80.2/−/−2.9/31.7/−
    T. rubrum ATCC 102188.7/24.8/24.86.5/17.6/23.52.7/5.6/11.11.0/2.0/5.3−/−/−>178.6/−/−8.4/15.8/−
  • a Highest test concentrations for compounds 1 to 7 were 198.1, 187.7, 178.3, 169.8, 162.1, 178.6, and 168.9 μM, respectively.

  • b Values are means from two independent experiments, each with two replicates; the run-to-run variability was within one- to twofold. −, not active at the highest test concentration.

  • c Some growth inhibition (25 to 49% inhibition) was observed at that concentration.

  • d Patient isolates were obtained during fluconazole therapy; isolate 1 (first isolate) and isolate 17 (last isolate) were azole resistant (35).

  • e Values are means from one experiment using two replicates.