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Design and synthesis of DPP-IV inhibitors lacking the electrophilic nitrile group.

Design and synthesis of DPP-IV inhibitors lacking the electrophilic nitrile group. Research Abstract Details 

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  • Design and synthesis of DPP-IV inhibitors lacking the electrophilic nitrile group. Abstract Text:

    takashi kondoTakashi Kondo,takahiro nekadoTakahiro Nekado,isamu sugimotoIsamu Sugimoto,kenya ochiKenya Ochi,shigeyuki takaiShigeyuki Takai,atsushi kinoshitaAtsushi Kinoshita,akira hatayamaAkira Hatayama,susumu yamamotoSusumu Yamamoto,katsuya kishikawaKatsuya Kishikawa,hisao nakaiHisao Nakai,masaaki todaMasaaki Toda,takashi kondoTakashi Kondo,takahiro nekadoTakahiro Nekado,isamu sugimotoIsamu Sugimoto,kenya ochiKenya Ochi,shigeyuki takaiShigeyuki Takai,atsushi kinoshitaAtsushi Kinoshita,akira hatayamaAkira Hatayama,susumu yamamotoSusumu Yamamoto,katsuya kishikawaKatsuya Kishikawa,hisao nakaiHisao Nakai,masaaki todaMasaaki Toda,

    A series of (4beta-substituted)-l-prolylpyrrolidine analogs lacking the electrophilic nitrile function were synthesized and their dipeptidyl peptidase IV (DPP-IV) inhibitory activity and duration of ex vivo activity were evaluated. Structural optimization of a N-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine analog 8, which was found by high-speed analog synthesis, was carried out to improve the potency and duration of action. A representative compound 26 was evaluated to assess its effect on the plasma glucose level after the oGTT (oral glucose tolerance test) in normal rats. Structure-activity relationships (SAR) are also presented.

    Design and synthesis of DPP-IV inhibitors lacking the electrophilic nitrile group. Publishing Authors By Initials

    t kondoT Kondo,t nekadoT Nekado,i sugimotoI Sugimoto,k ochiK Ochi,s takaiS Takai,a kinoshitaA Kinoshita,a hatayamaA Hatayama,s yamamotoS Yamamoto,k kishikawaK Kishikawa,h nakaiH Nakai,m todaM Toda,t kondoT Kondo,t nekadoT Nekado,i sugimotoI Sugimoto,k ochiK Ochi,s takaiS Takai,a kinoshitaA Kinoshita,a hatayamaA Hatayama,s yamamotoS Yamamoto,k kishikawaK Kishikawa,h nakaiH Nakai,m todaM Toda,

    For similar abstracts research abstracts see: abstracts research

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    Design and synthesis of DPP-IV inhibitors lacking the electrophilic nitrile group. Journal Published:

    PUBLICATION TYPE: Journal Article

    Journal: Bioorganic & medicinal chemistry

    VOLUME: 16

    Page Numbers: 1613-31

    Journal Abbreviation: Bioorg. Med. Chem.

    ISSN: 1464-3391

    DAY: 17

    MONTH: 11

    YEAR: 2007

    Design and synthesis of DPP-IV inhibitors lacking the electrophilic nitrile group. Information

    Number of References:

    LANGUAGE: eng

    NlmUniqueID: 9413298

    Design and synthesis of DPP-IV inhibitors lacking the electrophilic nitrile group. Keywords Mesh Terms:

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    Grant and Affiliation Information for Design and synthesis of DPP-IV inhibitors lacking the electrophilic nitrile group.

    AFFILIATION: Minase Research Institute, Ono Pharmaceutical Co., Ltd, 3-1-1 Sakurai, Shimamoto, Mishima, Osaka 618-8585, Japan.

    Country: England

    England Research Publication

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    MEDLINETA: Bioorg Med Chem

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