Carbon analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.


:A new series of triazole compounds possessing a carbon atom in place of a sulfur atom were efficiently synthesized and their in vitro antifungal activities were investigated. The carbon analogs showed excellent in vitro activity against Candida, Cryptococcus, and Aspergillus species. The MICs of compound 1c against C. albicans ATCC24433, C. neoformans TIMM1855, and A. fumigatus ATCC26430 were 0.016, 0.016, and 0.125 microg/mL, respectively (MICs of fluconazole: 0.5, >4, and >4 microg/mL; MICs of itraconazole: 0.125, 0.25, and 0.25 microg/mL).


Bioorg Med Chem Lett


Uchida T,Somada A,Kagoshima Y,Konosu T,Oida S




Has Abstract


2008-12-15 00:00:00














  • Efficient one-pot cyclization/folding of Rhesus θ-defensin-1 (RTD-1).

    abstract::We report an efficient approach for the chemical synthesis of Rhesus θ-defensin-1 (RTD-1) using Fmoc-based solid-phase peptide synthesis in combination with an intramolecular version of native chemical ligation. The corresponding linear thioester precursor was cyclized and folded in a one-pot reaction using reduced gl...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Aboye TL,Li Y,Majumder S,Hao J,Shekhtman A,Camarero JA

    更新日期:2012-04-15 00:00:00

  • Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs.

    abstract::In an effort to discover potent antitumor agents, a series of novel C-7-heteroaryl-substituted camptothecin derivatives were designed and synthesized via microwave-promoted Suzuki coupling reaction. These analogs were then assessed for cytotoxicity against three human tumor cell lines, A549, HCT116, HT-29, and inhibit...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Wang L,Huang Y,Zhang J,Tong L,Chen Y,Lu W,Huang Q

    更新日期:2014-03-15 00:00:00

  • Synthesis of 2-methyl-1,4-naphthoquinones with higher gamma-glutamyl carboxylase activity than MK-4 both in vitro and in vivo.

    abstract::Vitamin K is the collective term for compounds that share a 2-methyl-1,4-naphthoquinone ring, but differ in the side-chain at the 3-position. We synthesized novel 2-methyl-1,4-naphthoquinone derivatives with different side chain length at the 3-position. Derivatives with C-14 and C-16 tails showed the highest in vitro...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Vermeer C,van 't Hoofd C,Knapen MHJ,Xanthoulea S

    更新日期:2017-01-15 00:00:00

  • Synthesis and evaluation of 1-(quinoliloxypropyl)-4-aryl piperazines for atypical antipsychotic effect.

    abstract::A series of 1-(quinoliloxypropyl)-4-aryl-piperazines has been synthesized and the target compounds evaluated for atypical antipsychotic activity in apomorphine induced mesh climbing and stereotypic behaviour in mice. The 8-hydroxyquinoline ether derivative 14 has emerged as an important lead compound showing a potenti...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Bali A,Malhotra S,Dhir H,Kumar A,Sharma A

    更新日期:2009-06-01 00:00:00

  • TR-FRET binding assay targeting unactivated form of Bruton's tyrosine kinase.

    abstract::Bruton's Tyrosine Kinase (BTK) is one of the crucial kinases for the B cell maturation and mast cell activation, and specific inhibitors of BTK are considered to be attractive targets in drug discovery research. In this Letter, we have designed and synthesized a new fluorescent probe for TR-FRET-based high-throughput ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Asami T,Kawahata W,Sawa M

    更新日期:2015-01-01 00:00:00

  • Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series.

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Petrov KG,Zhang YM,Carter M,Cockerill GS,Dickerson S,Gauthier CA,Guo Y,Mook RA Jr,Rusnak DW,Walker AL,Wood ER,Lackey KE

    更新日期:2006-09-01 00:00:00

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Beck JP,Curry MA,Chorvat RJ,Fitzgerald LW,Gilligan PJ,Zaczek R,Trainor GL

    更新日期:1999-04-19 00:00:00

  • Electrochemical and peroxidase oxidation study of N'-hydroxyguanidine derivatives as NO donors.

    abstract::The electrochemical properties of a series of N-substituted-N'-hydroxyguanidines were studied. Two oxidation potentials of each compound were obtained by cyclic voltammetry. The E(ox1) values were from 0.51 to 0.62V, while the E(ox2) values were from 1.14 to 1.81V in acetonitrile solution. Next, their enzymatic contro...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Cai T,Xian M,Wang PG

    更新日期:2002-06-03 00:00:00

  • Synthesis and investigations into the anticancer and antibacterial activity studies of β-carboline chalcones and their bromide salts.

    abstract::A series of sixteen β-carbolines, bearing chalcone moiety at C-1 position, were prepared from easily accessible 1-acetyl-β-carboline and various aldehydes under basic conditions followed by N2-alkylation using different alkyl bromides. The prepared compounds were evaluated for in vitro cytotoxicity against a panel of ...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Venkataramana Reddy PO,Hridhay M,Nikhil K,Khan S,Jha PN,Shah K,Kumar D

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  • Towards new antibiotics targeting bacterial transglycosylase: Synthesis of a Lipid II analog as stable transition-state mimic inhibitor.

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Wang X,Krasnova L,Wu KB,Wu WS,Cheng TJ,Wong CH

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Eljabu F,Dhruval J,Yan H

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Patel P,Anumolu JR,Powell WS,Rokach J

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  • Synthesis of carbon-11 and fluorine-18 labeled N-acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives as new potential PET AMPA receptor ligands.

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Gao M,Kong D,Clearfield A,Zheng QH

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  • Thalidomide analogs and PDE4 inhibition.

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


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  • 7-Oxopyrrolopyridine-derived DPP4 inhibitors-mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site.

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Shi J,Ray AS,Mathew JS,Anderson KS,Chu CK,Schinazi RF

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    journal_title:Bioorganic & medicinal chemistry letters

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Ionescu C,Sippelli S,Toupet L,Barragan-Montero V

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Gawaskar S,Schepmann D,Bonifazi A,Robaa D,Sippl W,Wünsch B

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Seward EM,Carlson E,Harrison T,Haworth KR,Herbert R,Kelleher FJ,Kurtz MM,Moseley J,Owen SN,Owens AP,Sadowski SJ,Swain CJ,Williams BJ

    更新日期:2002-09-16 00:00:00

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Gupte A,Buolamwini JK

    更新日期:2004-05-03 00:00:00

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Geldenhuys WJ,Lockman PR,McAfee JH,Fitzpatrick KT,Van der Schyf CJ,Allen DD

    更新日期:2004-06-21 00:00:00

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Brouillette WJ,Atigadda VR,Luo M,Air GM,Babu YS,Bantia S

    更新日期:1999-07-19 00:00:00

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Kozikowski AP,Simoni D,Roberti M,Rondanin R,Wang S,Du P,Johnson KM

    更新日期:1999-07-05 00:00:00

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    abstract::Two series of triamino pyrimidines and a series of triamino pyridines have been synthesized and their structure-activity relationships evaluated for activity at the H(4) receptor in competitive binding and functional assays. Small structural changes in these three hetereoaromatic cores influenced the functional activi...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Meduna SP,Savall BM,Cai H,Edwards JP,Thurmond RL,McGovern PM

    更新日期:2011-05-15 00:00:00