Literature DB >> 15324904

Substituted piperazines as novel dipeptidyl peptidase IV inhibitors.

Linda L Brockunier1, Jiafang He, Lawrence F Colwell, Bahanu Habulihaz, Huaibing He, Barbara Leiting, Kathryn A Lyons, Frank Marsilio, Reshma A Patel, Yohannes Teffera, Joseph K Wu, Nancy A Thornberry, Ann E Weber, Emma R Parmee.   

Abstract

Incorporation of a fluorophenyl beta-amino amide moiety into piperazine screening lead 2 has resulted in the discovery of a structurally novel series of potent and selective DP-IV inhibitors. Simplification of the molecule and incorporation of multiple fluorine atoms on the phenyl ring has provided low molecular weight analogs such as compound 32, which is a 19nM DP-IV inhibitor with >4000-fold selectivity over QPP.

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Year:  2004        PMID: 15324904     DOI: 10.1016/j.bmcl.2004.06.065

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  23 in total

1.  Crystal-structure studies of 4-phenyl-piperazin-1-ium 4-eth-oxy-benzoate monohydrate, 4-phenyl-piperazin-1-ium 4-meth-oxy-benzoate monohydrate, 4-phenyl-piperazin-1-ium 4-methyl-benzoate monohydrate and 4-phenyl-piperazin-1-ium tri-fluoro-acetate 0.12-hydrate.

Authors:  Ninganayaka Mahesha; Haruvegowda Kiran Kumar; Mehmet Akkurt; Hemmige S Yathirajan; Sabine Foro; Mohammed S M Abdelbaky; Santiago Garcia-Granda
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2022-06-10

2.  Molecular docking and 3D-QSAR studies on beta-phenylalanine derivatives as dipeptidyl peptidase IV inhibitors.

Authors:  Yan-Ke Jiang
Journal:  J Mol Model       Date:  2010-01-13       Impact factor: 1.810

3.  4-[Bis(4-fluoro-phen-yl)meth-yl]piperazin-1-ium bis-(trichloro-acetate) 0.4-hydrate.

Authors:  A S Dayananda; H S Yathirajan; Ulrich Flörke
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-03-07

4.  4-[Bis(4-fluoro-phen-yl)meth-yl]piperazin-1-ium 2-hy-droxy-benzoate 2-hy-droxy-benzoic acid monosolvate.

Authors:  A S Dayananda; H S Yathirajan; Ulrich Flörke
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-03-24

5.  1-Methyl-piperazine-1,4-diium dipicrate.

Authors:  Grzegorz Dutkiewicz; S Samshuddin; B Narayana; H S Yathirajan; Maciej Kubicki
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-01-15

6.  4-[Bis(4-fluorophenyl)methyl]piperazin-1-ium picrate.

Authors:  Richard Betz; Thomas Gerber; Eric Hosten; Alaloor S Dayananda; Hemmige S Yathirajan; Badiadka Narayana
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-09-14

7.  4-[Bis(4-fluorophenyl)methyl]piperazin-1-ium 2-(2-phenylethyl)benzoate.

Authors:  Richard Betz; Thomas Gerber; Eric Hosten; Alaloor S Dayananda; Hemmige S Yathirajan
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-09-30

8.  1-[Bis(4-fluoro-phen-yl)meth-yl]piperazine.

Authors:  A S Dayananda; Grzegorz Dutkiewicz; H S Yathirajan; A R Ramesha; Maciej Kubicki
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-08-31

9.  4-[Bis(4-fluoro-phen-yl)meth-yl]-1-[(2E)-3-phenyl-prop-2-en-1-yl]piperazin-1-ium 3-carb-oxy-propano-ate.

Authors:  Channappa N Kavitha; Hemmige S Yathirajan; Badiadka Narayana; Thomas Gerber; Benjamin van Brecht; Richard Betz
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-01-19

10.  1-{4-[Bis(4-fluoro-phen-yl)meth-yl]piperazin-1-yl}ethanone.

Authors:  A S Dayananda; H S Yathirajan; Amanda C Keeley; Jerry P Jasinski
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-06-27
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