Table 1.

In vitro antifungal activity of miconazole and analogues [2].

	R	X	Y	Z	C.a.(a)	M.c.	T.m.	T.r.	A.f.(b)
2a	H	0	2,4-Cl2	2,4-Cl2	10	<1	0.1	<1	10
2b	H	0	2,4-Cl2	2,6-Cl2	100	<1	0.1	0.1	10
2c	H	0	4-F	2,4-Cl2	100	10	<1	<1	10
2d	H	0	2,4-Cl2	4-F	100	10	10	10	10
2e	H	0	2,4-Cl2	2-F	100	10	10	10	100
2f	H	0	2,4-Cl2	2-Cl	100	10	0.1	0.1	10
2g	H	0	4-Cl	2,6-Cl2	10	100	10	10	100
2h	H	0	2,4-Cl2	4-Cl	100	0.1	0.01	0.1	<1
2i	H	0	4-Cl	2,4-Cl2	10	10	<1	0.1	10
2j	H	0	2-Cl	2,4-Cl2	100	<1	<1	<1	10
2k	H	0	4-Br	2-Cl	100	10	10	10	100
2l	H	0	4-Br	4-Cl	10	<1	0.1	0.1	<1
2m	H	0	4-F	4-Cl	100	<1	<1	<1	10
2n	H	0	4-F	2-Cl	100	100	10	<1	100
2o	H	0	4-Cl	2-Cl	100	100	10	10	100
2p	H	0	4-Cl	4-Cl	10	<1	0.1	0.1	10
2q	H	0	H	4-Cl	100	10	<1	<1	10
2r	H	0	H	H	>100	100	10	10	100
2s	H	0	4-Me	2,4-Cl2	100	100	10	10	100
2t	H	0	2-Me	2,4-Cl2	100	10	10	<1	10
2u	H	0	2,4-Cl2	2-Me	100	10	0.1	0.1	10
2v	H	0	2-Me	2,4-Cl2	100	<1	<1	<1	<1
2w	H	0	2,4-Cl2	3-MeO	100	10	10	10	100
2x	H	0	2,4-Cl2	4-MeO	100	10	10	10	100
2y	H	0	4-Cl	2-Me	100	100	10	10	100
2z	H	0	4-Me	2-Cl	100	100	10	10	100
2aa	H	0	4-Me	4-Cl	100	10	<1	<1	10
3a	Me	0	4-Cl	2,4-Cl2	>100	10	10	10	100
3b	Me	0	H	2,4-Cl2	>100	100	10	10	>100
3c	Me	0	4-Cl	4-Cl	100	100	10	10	100
5	H	NH	4-Cl	2-Cl	>100	100	100	100	ND(c)
tolnaftate					>100	>100	10	<1	>100
nystatin					333	ND	ND	ND	ND

^(a) Lowest concentration of total inhibition (μg/mL); ^(b) C.a.: Candida albicans; M.c.: Microsporum canis; T.m.: Trichophyton mentagrophytes;T.r.: Trichophyton rubrum; A.f.: Aspergillus fumigates

^(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; 2a: miconazole; 2b: isoconazole; 2h: econazole. ^(c) ND: not done.