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 Kondo,Takahiro Nekado,Isamu Sugimoto,Kenya Ochi,Shigeyuki Takai,Atsushi Kinoshita,Akira Hatayama,Susumu Yamamoto,Kazuhito Kawabata,Hisao Nakai,Masaaki Toda,Takashi Kondo,Takahiro Nekado,Isamu Sugimoto,Kenya Ochi,Shigeyuki Takai,Atsushi Kinoshita,Akira Hatayama,Susumu Yamamoto,Kazuhito Kawabata,Hisao Nakai,Masaaki Toda,Takashi Kondo,Takahiro Nekado,Isamu Sugimoto,Kenya Ochi,Shigeyuki Takai,Atsushi Kinoshita,Akira Hatayama,Susumu Yamamoto,Kazuhito Kawabata,Hisao Nakai,Masaaki 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 Kondo,T Nekado,I Sugimoto,K Ochi,S Takai,A Kinoshita,A Hatayama,S Yamamoto,K Kawabata,H Nakai,M Toda,T Kondo,T Nekado,I Sugimoto,K Ochi,S Takai,A Kinoshita,A Hatayama,S Yamamoto,K Kawabata,H Nakai,M Toda,T Kondo,T Nekado,I Sugimoto,K Ochi,S Takai,A Kinoshita,A Hatayama,S Yamamoto,K Kawabata,H Nakai,M Toda,

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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

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LANGUAGE: eng

NlmUniqueID: 9413298

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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

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MEDLINETA: Bioorg Med Chem

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