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1.
Bioorg Med Chem Lett ; 22(18): 5777-9, 2012 Sep 15.
Article in English | MEDLINE | ID: mdl-22902652

ABSTRACT

1-Thia-4b-aza-cyclopenta[b]fluorene-4,10-diones were synthesized and tested for in vitro antifungal activity against two pathogenic strains of fungi. Among them tested, many compounds showed good antifungal activity. The results suggest that 1-thia-4b-aza-cyclopenta[b]fluorene-4,10-diones would be antifungal agents.


Subject(s)
Antifungal Agents/chemical synthesis , Antifungal Agents/pharmacology , Fluorenes/pharmacology , Fungi/drug effects , Antifungal Agents/chemistry , Dose-Response Relationship, Drug , Fluorenes/chemical synthesis , Fluorenes/chemistry , Fungi/growth & development , Microbial Sensitivity Tests , Molecular Structure , Stereoisomerism , Structure-Activity Relationship
2.
Bioorg Med Chem Lett ; 22(1): 497-9, 2012 Jan 01.
Article in English | MEDLINE | ID: mdl-22115590

ABSTRACT

Pyrido[1,2-a]indole-1,4-diones and benzo[f]pyrido[1,2-a]indole-6,11-diones were synthesized and tested for in vitro antifungal activity against two pathogenic strains of fungi. Among them tested, many compounds showed good antifungal activity. The results suggest that pyrido[1,2-a]indole-1,4-diones and benzo[f]pyrido[1,2-a]indole-6,11-diones would be potent antifungal agents.


Subject(s)
Antifungal Agents/pharmacology , Carbolines/chemical synthesis , Chemistry, Pharmaceutical/methods , Aspergillus flavus/metabolism , Aspergillus niger/metabolism , Candida albicans/metabolism , Carbolines/pharmacology , Drug Design , Fungi/drug effects , Indoles/chemistry , Microbial Sensitivity Tests , Models, Chemical , Saccharomyces cerevisiae/metabolism , Time Factors
3.
Bioorg Med Chem Lett ; 22(1): 500-3, 2012 Jan 01.
Article in English | MEDLINE | ID: mdl-22113112

ABSTRACT

6,7-Bis(arylthio)-quinazoline-5,8-dione and furo[2,3-f]quinazolin-5-ol derivatives were synthesized and tested for in vitro antifungal activity against Candida, Aspergillus species, and Cryptococcus neoformans. Among them tested, many of furo[2,3-f]quinazolin-5-ols and 6,7-bis(arylthio)-quinazoline-5,8-diones showed good antifungal activity. The compounds completely inhibited the growth of all against Candida and Aspergillus species tested at the MIC level of 12.5µg/mL. The results suggest that furo[2,3-f]quinazolin-5-ols and 6,7-bis(arylthio)-quinazoline-5,8-diones would be promising antifungal agents.


Subject(s)
Antifungal Agents/pharmacology , Aspergillus/metabolism , Candida/metabolism , Chemistry, Pharmaceutical/methods , Cryptococcus neoformans/metabolism , Dose-Response Relationship, Drug , Drug Design , Fluconazole/chemistry , Microbial Sensitivity Tests , Models, Chemical , Quinazolines/chemistry , Structure-Activity Relationship , Sulfhydryl Compounds/chemistry
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