Table 3.
In vitro antifungal and antibacterial activities and in vivo antifungal data of miconazole analogues containing a dioxolane scaffold [8].
 | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| X | Y | n | M.c.(a,b) | T.m. | T.r. | Ph.v.(c) | Cr.n. | C.tr. | C.a. | Muc. | A.f. | Rat(d,e) | Guinea Pig (f) | |
| 9d | 4-Cl | 2-Cl2 | 0 | 10 | <1 | <1 | 100 | 10 | >100 | >100 | 100 | 100 | NT | NT |
| 9e | 4-Cl | 2,4-Cl2 | 0 | 10 | <1 | <1 | 100 | 10 | >100 | 100 | 100 | 100 | 1/2 | 2/2 |
| 9f | 2,4-Cl2 | H | 0 | <1 | <1 | <1 | 100 | 100 | >100 | 100 | 100 | <1 | 0/2 | NT |
| 9g | 2,4-Cl2 | 2-Cl | 0 | 10 | <1 | <1 | 100 | <1 | 100 | 100 | 100 | 100 | - | NT |
| 9h | 2,4-Cl2 | 4-Cl | 0 | <1 | <1 | <1 | 100 | <1 | 10 | 100 | 10 | <1 | NT | 1/2 |
| 9i | 2,4-Cl2 | 2,4-Cl2 | 0 | 10 | <1 | <1 | 100 | <1 | >100 | >100 | 10 | <1 | 2/2 | NT |
| 9j | 2,4-Cl2 | 4-Br | 0 | <1 | <1 | <1 | 100 | <1 | 10 | 100 | 10 | <1 | 0/2 | 3/4 |
| 9k | 2,4-Cl2 | H | 1 | <1 | <1 | <1 | 100 | <1 | 10 | 100 | 10 | <1 | 0/2 | 2/2 |
| 9l | 2,4-Cl2 | 4-Cl | 1 | <1 | <1 | <1 | 100 | 1 | 10 | 10 | 10 | 10 | 0/2 | 2/2 |
| 9m | 2,4-Cl2 | 4-Br | 1 | <1 | <1 | <1 | 100 | <1 | >100 | 10 | <1 | 10 | 0/2 | NT |
| 9n | 2,4-Cl2 | 4-Ph | 1 | 10 | <1 | <1 | >100 | 100 | >100 | >100 | 10 | 100 | 0/2 | NT |
| 9o | 2,4-Cl2 | 4-Ph | 2 | <1 | <1 | <1 | >100 | 10 | >100 | >100 | >100 | 10 | 0/2 | NT |
| 2a | miconazole | 1 | <1 | <1 | 100 | 1 | 100 | 10 | >100 | 10 | 0/6 | 4/13 | ||
(a) Lowest concentration of total inhibition (μg/mL); M.c.: Microsporum canis; T.m.: Trichophyton mentagrophytes; T.r.: Trichophyton rubrum; Ph.v.: Phialophora verrucosum; Cr.n.: Cryptococcus neoformans; C.tr.: Candida tropicalis; C.a.: Candida albicans;Muc.: Mucor species; A.f.: Aspergillus fumigatus; (b) Figures proceeded by "<" represent the lowest dose level tested (µg/mL) with complete inhibition; (c) Figures proceeded by ">" denoted partial growth at 100 µg/mL; (d) Oral treatment (10 mg/kg) of vaginal candidiasis by C.albicans in rats; Ratio of animals cured/infected; (e) NT = not tested; (f) Oral treatment (10 mg/kg) of cutaneous candidiasis by C.albicans in guinea pigs; Ratio of animals cured/infected.