Amide analogs of antifungal dioxane-triazole derivatives: Synthesis and in vitro activities

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 7, 2009, Pages 2013-2017

  Uchida, Takuya ^a   Kagoshima, Yoshiko ^a   Konosu, Toshiyuki ^a  

^a DAIICHI SANKYO CO   (Japan)

Author keywords

Acid stability; Amide analog; Antifungal; Triazole

Indexed keywords

4 [4 [5 [2 (2,4 DIFLUOROPHENYL) 2 HYDROXY 1 METHYL 3 (1H 1,2,4, TRIAZOL 1 YL)PROPYLTHIO] 1,3 DIOXAN 2 YL] 1,3 BUTADIENYL] 3 FLUOROBENZONITIRLE; AMIDE; DIOXANE DERIVATIVE; FLUCONAZOLE; ITRACONAZOLE; TRIAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

ANTIFUNGAL ACTIVITY; ARTICLE; ASPERGILLUS FLAVUS; ASPERGILLUS FUMIGATUS; CANDIDA ALBICANS; CANDIDA TROPICALIS; CONTROLLED STUDY; CRYPTOCOCCUS NEOFORMANS; DRUG SYNTHESIS; IN VITRO STUDY; MINIMUM INHIBITORY CONCENTRATION; NONHUMAN; STRUCTURE ACTIVITY RELATION;

AMIDES; ANTIFUNGAL AGENTS; BENZAMIDES; CANDIDA; DIOXANES; MICROBIAL SENSITIVITY TESTS; TRIAZOLES;

ASPERGILLUS; ASPERGILLUS FUMIGATUS; CANDIDA; CANDIDA ALBICANS;

EID: 61849154264     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.02.036     Document Type: Article

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8. 1H NMR spectra. The trans isomers showed characteristic signals of the axial methylene protons on the C4 and C6 positions in the 1,3-dioxane ring with large coupling constants (triplet, J = ca. 11 Hz). In contrast, the corresponding signals of cis isomers appeared as multiplets.
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11. 4S: C, 60.90; H, 4.60; N, 11.84; S, 5.42; F, 6.42. Found: C, 61.14; H, 4.35; N, 11.58; S, 5.30; F, 6.39.
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