• Journal of the Korean Applied Science and Technology
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• v.11 no.2
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• pp.105-111
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• 1994

Intermediates, 1-benzyl-2-substituted-3-carboxaldehyde[I]-[II], were prepared by the reaction of 2-substituted indole-3-carboxaldehyde with benzyl chloride. Indolylacrylophenone derivatives[III]-[X] were prepared from 1-benzyl-2-substituted-3-carboxaldehyde with acetophenone derivatives. They are as follows; 3-(1'-benzylindole-3'-yl)-1acrylophenone [III] 3-(1'-benzylindole-3-yl)-1(p-methoxy)acrylophenone [IV] 3-(1'-benzylindole-3-yl)-1(p-bromo)acrylophenone [V] 3-(1'-benzylindole-3-yl)-1(p-chloro)acrylophenone [VI] 3-(1'-benzyl-2'-methylindole-3'-yl)-1-acrylophenone [VII] 3-(1'-benzyl-2'-methylindole-3'-yl)-1-(p-methoxy)acrylophenone [VIII] 3-(1'-benzyl-2'-methylindole-3'-yl)-1-(p-bromo)acrylophenone [VIII] 3-(1'-benzyl-2'-methylindole-3'-yl)-1-(p-chloro)acrylophenone [X]

• Archives of Pharmacal Research
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• v.16 no.4
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• pp.327-330
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• 1993

A series of 2-chloro and 2-bromo-3-(substituted)-1, 4-naphthalenedione derivatives (1-25) were tested for antifungal and antibacterial activities in vitro against Candida albicans 10231 aand Local, Aspergillus niger KCTC 1231, Tricophyton mentagrophytes KCTC 6085, Fusarium oxysporium KTCC 6501, Bacillus subtilis ATCC 6633, Pseudomonas arruginosa NCTC 10490, Staphylococcus aureus ATCC 6358p, Escherichia coli NIHJ and Acinetobacter baumanii Local. The MiC values were determined by twofold afar diution/streak method. Among thee derivatives, 1, 9, 20, 21, 23 and 25 showed more potent antifungal activities than fluconazole. 20 and 23 completely inhibited the gorwth of fungi, such as Candida albicans, Aspegillus niger, Ticophyton mentagrophytes and fusarium oxysporium, at $3.2\;\mu{g/ml}$. Also some derivatives had the antibacterial activities against Gram-positive bacteria.

• YAKHAK HOEJI
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• v.36 no.2
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• pp.110-114
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• 1992

In order to evaluate the antimicrobial effect of 2, 3-substituted-1, 4-naphthoquinone derivatives, we newly synthesized several 2-chloro, 2-bromo and 2-hydroxy-1, 4-naphthoquinones and subjected to antibacterial and antifungal activities, in vitro, against Escherichia coli NIHJ, Staphylococcus aureus ATCC6538p, Candida albicans 10231, Aspergillus niger 1231 and Tricophyton mentagrophytes 6085. Among these derivatives 3, 9, 18 and 23 showed the potent antibacterial activities. 18, 23 and 28 have the antifungal activities. However, these compounds have no significant hemolytic activity at concentrations higher than that required for showing the antibacterial and antifungal activities.

• Archives of Pharmacal Research
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• v.16 no.2
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• pp.161-163
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• 1993

In order to evaluate the antimicrobial effect of 2,3-disubstituted-1,4-naphthalenedione derivatives, we synthesized several 2-chloro, 2-bromo and 2-hydroxy-3(substituted)-1, 4-naphthalene-diones (1-25). These derivatives were tested for antifugal and antibacterial activities, in vitro, against Candida albicans 10231 and local, Aspergillus niger KCTC 1231, Tricophyton mentagrophytes KCTC 6085, Baciilus subtilis ACTT 6633, Pseudomonas aeruginsa NCTC 10490, Staphylococcus aureus ATCC 6538P, Escherichia coli NIHJ. The MIC values were determined by the two-fold agar dilution/strea method. Among these derivatives, 4, 5 and 6 showed the potent antifungal activities. Also 5 and 6 had the antibacterial activities. 5 with (1,2,4-triazolyl)-amino moirty was the most effective in preventing the growth of fungi, such as Candida albicans, Aspergillus niger and Tricophyton mentagrophytes.

• Archives of Pharmacal Research
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• v.15 no.3
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• pp.263-268
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• 1992

In order to evaluate the antimicrobial effect of 2, 3-disubstitued-1, 4-naphtoquinone derivatives we newly synthesized several 2-bromo-3-(substituted)-1, 4 naphthoquninones. Amination reaction of 2, 3-dihalo-1, 4 naphthoquinones with aryl and aliphatic amines in ethanol gave 2-halo-3-(N-alkyl or N-aryl)1, 4-naphtoquinone derivatives (1a, b-10a, b) i 60% 90%) yield. These derivatives subjected to antibacterial and antifungal activities. in vitro, against Bacilllus subtilis ATCC 6633 Candida albicans 10231 and local, Psudomonas aeruginosa NCTC10490, Staphylococcus aureus ATCC 6538p. Escherichia coli NIHJ Aspergillus niger KCTC 1231, Tricophyton mentagrophytes KCTC 6085. Among these derivatives 1b, 6b and 7a showed the potent antibacterial activities 1b, 8b and 9b have derivatives, 1b, 6b and 7a showed the potent antibacterial activities. 1b, 8b and 9b have the antifungal activities. 1b is most effective in preventing the growth of Bacillus subtilis and Psudomonas aeruginosa. Candida albicans. Aspergillus niger. Tricophyton mentagrophytes. The several of these compounds demonstrated a broad spectrum of activities in vitro.