Document Detail

Synthesis and antifungal activities of R-102557 and related dioxane-triazole derivatives.
MedLine Citation:
PMID:  10823709     Owner:  NLM     Status:  MEDLINE    
Novel triazole compounds with a dioxane ring were synthesized. Condensation of the diol precursor 10 with various aromatic aldehydes 11-13 under acidic conditions afforded a series of dioxane-triazole compounds 14-16. The antifungal activities of the compounds 14-16 were evaluated in vivo in mice infection models against Candida and Aspergillus species. High activities were seen for the derivatives with one or two double bond(s) and an aromatic ring substituted with an electron-withdrawing group in the side chain. Among the derivatives, R-102557 (16R: Ar=4-(2,2,3,3-tetrafluoropropoxy)phenyl) showed excellent in vivo activities against Candida, Aspergillus and Cryptococcus species. It also showed high tolerance in a preliminary toxicity study in rats.
S Oida; Y Tajima; T Konosu; Y Nakamura; A Somada; T Tanaka; S Habuki; T Harasaki; Y Kamai; T Fukuoka; S Ohya; H Yasuda
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Chemical & pharmaceutical bulletin     Volume:  48     ISSN:  0009-2363     ISO Abbreviation:  Chem. Pharm. Bull.     Publication Date:  2000 May 
Date Detail:
Created Date:  2000-09-20     Completed Date:  2000-09-20     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0377775     Medline TA:  Chem Pharm Bull (Tokyo)     Country:  JAPAN    
Other Details:
Languages:  eng     Pagination:  694-707     Citation Subset:  IM    
Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd., Tokyo, Japan.
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MeSH Terms
Antifungal Agents / chemical synthesis*,  pharmacology,  toxicity
Aspergillosis / drug therapy,  microbiology
Aspergillus flavus
Aspergillus fumigatus
Cryptococcosis / microbiology
Cryptococcus neoformans
Dioxanes / chemical synthesis*,  pharmacology,  toxicity
Mass Spectrometry
Microbial Sensitivity Tests
Rats, Inbred F344
Spectrophotometry, Infrared
Structure-Activity Relationship
Triazoles / chemical synthesis*,  pharmacology,  toxicity
Reg. No./Substance:
0/Antifungal Agents; 0/Dioxanes; 0/R 102557; 0/Triazoles

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