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Discovery of long-acting N-(cyanomethyl)-N-alkyl-l-prolinamide inhibitors of dipeptidyl peptidase IV.

Discovery of long-acting N-(cyanomethyl)-N-alkyl-l-prolinamide inhibitors of dipeptidyl peptidase IV. Research Abstract Details 

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  • Discovery of long-acting N-(cyanomethyl)-N-alkyl-l-prolinamide inhibitors of dipeptidyl peptidase IV. 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,kazuhito kawabataKazuhito Kawabata,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,kazuhito kawabataKazuhito Kawabata,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,kazuhito kawabataKazuhito Kawabata,hisao nakaiHisao Nakai,masaaki todaMasaaki Toda,

    Details of structure-activity relationships (SAR) for P2 moiety of a P1 2-cyanopyrrolidine dipeptidyl peptidase IV (DPP-IV) inhibitor 4a including stereochemistry are presented. Based on this information, a series of P1 (N-alkyl)aminoacetonitrile analogs 9-20 possessing optimal P2 structure were synthesized and evaluated as inhibitors of DPP-IV. Among them, a representative compound 11, N-(cyanomethyl)-N-ethyl-l-prolinamide, was further evaluated to determine its effect on the plasma glucose level. Also 4a, 10, and 11 were evaluated for their isozyme selectivity to predict their safety problems.

    Discovery of long-acting N-(cyanomethyl)-N-alkyl-l-prolinamide inhibitors of dipeptidyl peptidase IV. 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 kawabataK Kawabata,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 kawabataK Kawabata,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 kawabataK Kawabata,h nakaiH Nakai,m todaM Toda,

    For similar abstracts research abstracts see: abstracts research

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    Discovery of long-acting N-(cyanomethyl)-N-alkyl-l-prolinamide inhibitors of dipeptidyl peptidase IV. Journal Published:

    PUBLICATION TYPE: Journal Article

    Journal: Bioorganic & medicinal chemistry

    VOLUME: 16

    Page Numbers: 190-208

    Journal Abbreviation: Bioorg. Med. Chem.

    ISSN: 1464-3391

    DAY: 5

    MONTH: 10

    YEAR: 2007

    Discovery of long-acting N-(cyanomethyl)-N-alkyl-l-prolinamide inhibitors of dipeptidyl peptidase IV. Information

    Number of References:

    LANGUAGE: eng

    NlmUniqueID: 9413298

    Discovery of long-acting N-(cyanomethyl)-N-alkyl-l-prolinamide inhibitors of dipeptidyl peptidase IV. Keywords Mesh Terms:

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    Chemical & Substance for Abstract: Discovery of long-acting N-(cyanomethyl)-N-alkyl-l-prolinamide inhibitors of dipeptidyl peptidase IV. Information

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    Grant and Affiliation Information for Discovery of long-acting N-(cyanomethyl)-N-alkyl-l-prolinamide inhibitors of dipeptidyl peptidase IV.

    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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