Synthesis and SAR studies of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists.


:Synthesis and structure-activity relationships (SAR) of a novel series of vasopressin V(1b) (V(3)) antagonists are described. 2-(4-Oxo-2-aryl-quinazolin-3(4H)-yl)acetamides have been identified with low nanomolar affinity for the V(1b) receptor and good selectivity with respect to related receptors V(1a), V(2) and oxytocin (OT). Optimised compound 12j demonstrates a good pharmacokinetic profile and activity in a mechanistic model of HPA dysfunction.


Bioorg Med Chem Lett


Napier SE,Letourneau JJ,Ansari N,Auld DS,Baker J,Best S,Campbell-Wan L,Chan JH,Craighead M,Desai H,Goan KA,Ho KK,Hulskotte EG,MacSweeney CP,Milne R,Morphy JR,Neagu I,Ohlmeyer MH,Peeters AW,Presland J,Riviello C,




Has Abstract


2011-03-15 00:00:00














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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Fournier PA,Arbour M,Cauchon E,Chen A,Chefson A,Ducharme Y,Falgueyret JP,Gagné S,Grimm E,Han Y,Houle R,Lacombe P,Lévesque JF,MacDonald D,Mackay B,McKay D,Percival MD,Ramtohul Y,St-Jacques R,Toulmond S

    更新日期:2012-04-15 00:00:00

  • Discovery of 5-substituted-N-arylpyridazinones as inhibitors of p38 MAP kinase.

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Jerome KD,Hepperle ME,Walker JK,Xing L,Devraj RV,Benson AG,Baldus JE,Selness SR

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Aridoss G,Amirthaganesan S,Jeong YT

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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: Liu YR,Luo JZ,Duan PP,Shao J,Zhao BX,Miao JY

    更新日期:2012-11-15 00:00:00

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Schnatbaum K,Schaudt M,Stragies R,Pfeifer JR,Gibson C,Locardi E,Scharn D,Richter U,Kalkhof H,Dinkel K,Zischinsky G

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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 XJ,Gong DL,Wang JD,Zhang J,Liu CX,Xiang WS

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Sharma VM,Adi Seshu KV,Chandra Sekhar V,Madan S,Vishnu B,Babu PA,Vamsee Krishna C,Sreenu J,Ravi Krishna V,Venkateswarlu A,Rajagopal S,Ajaykumar R,Kumar TS

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Devillers I,Dive G,De Tollenaere C,Falmagne B,de Wergifosse B,Rees JF,Marchand-Brynaert J

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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


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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: Isomura S,Ito K,Haruna M

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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: Jeung CS,Song JB,Kim YH,Suh J

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Blackburn C,Barrett C,Brunson M,Chin J,England D,Garcia K,Gigstad K,Gould A,Gutierrez J,Hoar K,Rowland RS,Tsu C,Ringeling J,Wager K,Xu H

    更新日期:2014-12-01 00:00:00

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Nazir Y,Saeed A,Rafiq M,Afzal S,Ali A,Latif M,Zuegg J,Hussein WM,Fercher C,Barnard RT,Cooper MA,Blaskovich MAT,Ashraf Z,Ziora ZM

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Smith G,Ruhland T,Mikkelsen G,Andersen K,Christoffersen CT,Alifrangis LH,Mørk A,Wren SP,Harris N,Wyman BM,Brandt G

    更新日期:2004-08-02 00:00:00

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    journal_title:Bioorganic & medicinal chemistry letters

    pub_type: 杂志文章


    authors: Sridhar J,Sfondouris ME,Bratton MR,Nguyen TL,Townley I,Klein Stevens CL,Jones FE

    更新日期:2014-01-01 00:00:00