New nemadectin congeners with acaricidal and nematocidal activity from Streptomyces microflavus neau3 Y-3.


:Two nemadectin congeners 1 and 2 were isolated from the fermentation broth of a mutant strain (Y-3) of Streptomyces microflavus neau3. Their structures were determined on the basis of extensive spectroscopic analysis and comparison with data from the literature. Compound 2 possessed a 5-membered ring lactone that is unprecedented among known milbemycins and avermectins. Both compounds 1 and 2 exhibited potent acaricidal activity and nematocidal activity. Especially, compound 2 demonstrated impressive acaricidal activity against adult mites with an IC50 of 2.3±0.9 μg/mL and mite eggs with an IC50 of 17.5±2.1 μg/mL and nematocidal activity against Caenorhabditis elegans with an IC50 of 0.7±0.2 μg/mL, which are higher than those of nemadectin and the known commercial acaricide and nematocide milbemycin A3/A4.


Bioorg Med Chem Lett


Yang LY,Wang JD,Zhang J,Xue CY,Zhang H,Wang XJ,Xiang WS




Has Abstract


2013-10-15 00:00:00














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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Zhang RH,Wang S,Luo RH,Zhou M,Zhang H,Xu GB,Zhao YL,Li YJ,Wang YL,Yan G,Liao SG,Zheng YT,Li R

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Panda S,Kar A,Sharma P,Sharma A

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Agarwal S,Schroeder C,Schlechtingen G,Braxmeier T,Jennings G,Knölker HJ

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Egle I,MacLean N,Demchyshyn L,Edwards L,Slassi A,Tehim A

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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: Mittapalli GK,Zhao F,Jackson A,Gao H,Lee H,Chow S,Kaur MP,Nguyen N,Zamboni R,McKelvy J,Wong-Staal F,Macdonald JE

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  • Design checkpoint kinase 2 inhibitors by pharmacophore modeling and virtual screening techniques.

    abstract::Damage to DNA is caused by ionizing radiation, genotoxic chemicals or collapsed replication forks. When DNA is damaged or cells fail to respond, a mutation that is associated with breast or ovarian cancer may occur. Mammalian cells control and stabilize the genome using a cell cycle checkpoint to prevent damage to DNA...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


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    abstract::Topical microbicides offer women the opportunity to protect themselves from sexual HIV transmission under their own control. A series of poly[styrene-alt-(maleic anhydride)] derivatives were prepared by amidation or hydrolysis of the anhydride moiety. The derivatives were shown to be of low cell toxicity and effective...

    journal_title:Bioorganic & medicinal chemistry letters

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    authors: Fang W,Cai Y,Chen X,Su R,Chen T,Xia N,Li L,Yang Q,Han J,Han S

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  • Synthesis of ketomethylene amino pseudopeptide analogues via reductive amination of glyoxals derived from alpha-amino acids.

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Groarke M,Hartzoulakis B,McKervey MA,Walker B,Williams CH

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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

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    journal_title:Bioorganic & medicinal chemistry letters

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  • 2-(Anilino)imidazolines and 2-(benzyl)imidazoline derivatives as h5-HT1D serotonin receptor ligands.

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    journal_title:Bioorganic & medicinal chemistry letters

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    authors: Prisinzano T,Dukat M,Law H,Slassi A,MacLean N,DeLannoy I,Glennon RA

    更新日期:2004-09-20 00:00:00

  • Diaryl piperidines as CB1 receptor antagonists.

    abstract::The syntheses and SAR investigations of novel CB(1) receptor antagonists based on a 1,2-diaryl piperidine core have been described. Optimization of this core afforded a compound with robust in vivo potency by reducing food intake in a mouse DIO model. ...

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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

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    journal_title:Bioorganic & medicinal chemistry letters

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    journal_title:Bioorganic & medicinal chemistry letters

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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


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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: Wang W,Devasthale P,Wang A,Harrity T,Egan D,Morgan N,Cap M,Fura A,Klei HE,Kish K,Weigelt C,Sun L,Levesque P,Li YX,Zahler R,Kirby MS,Hamann LG

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Micheli F,Bonanomi G,Braggio S,Capelli AM,Damiani F,Di Fabio R,Donati D,Gentile G,Hamprecht D,Perini O,Petrone M,Tedesco G,Terreni S,Worby A,Heidbreder C

    更新日期:2008-02-01 00:00:00

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    abstract::Two new cyclic octapeptides, mariannamides A (1) and B (2), have been isolated from Mariannaea elegans NBRC102301, a Pinus densiflora-derived filamentous fungus. Their structures were elucidated to be cyclo-(l-Leu1-l-Pro1-l-Pro2-l-Leu2-l-Ile1-l-Pro3-l-Val1-l-Ile2) and cyclo-(l-Leu1-l-Pro1-l-Pro2-l-Leu2-l-Ile1-l-Pro3-l...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Ishiuchi K,Hirose D,Kondo T,Watanabe K,Terasaka K,Makino T

    更新日期:2020-02-15 00:00:00

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    abstract::A variety of new prodrugs of 2'-methyl cytidine based on acyloxy ethylamino phosphoramidates have been synthesized and tested in vitro and in vivo for their biological activity. Compared with the parent drug a 10- to 20-fold increase in formation of nucleotide triphosphate in rat and human hepatocytes could be achieve...

    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Donghi M,Attenni B,Gardelli C,Marco AD,Fiore F,Giuliano C,Laufer R,Leone JF,Pucci V,Rowley M,Narjes F

    更新日期:2009-03-01 00:00:00