Literature DB >> 15713382

Synthesis and evaluation of pyrazolidine derivatives as dipeptidyl peptidase IV (DP-IV) inhibitors.

Jin Hee Ahn1, Jin Ah Kim, Hye-Min Kim, Hyuk-Man Kwon, Sun-Chul Huh, Sang Dal Rhee, Kwang Rok Kim, Sung-Don Yang, Sung-Dae Park, Jae Mok Lee, Sung Soo Kim, Hyae Gyeong Cheon.   

Abstract

A new series of pyrazolidine derivatives was synthesized and evaluated for their ability to inhibit dipeptidyl peptidase IV (DP-IV). Compound 9i was the most active in this series, exhibited IC50 value of 1.56 microM and ED50 value of 80 mg/kg (in vivo DP-IV inhibition; po).

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Year:  2005        PMID: 15713382     DOI: 10.1016/j.bmcl.2005.01.020

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


  4 in total

1.  Synthesis of spiro-fused pyrazolidoylisoxazolines.

Authors:  Kathryn G Guggenheim; Jeffrey D Butler; Phillip P Painter; Beth A Lorsbach; Dean J Tantillo; Mark J Kurth
Journal:  J Org Chem       Date:  2011-06-22       Impact factor: 4.354

2.  Stereoselective synthesis of cis- or trans-3,5-disubstituted pyrazolidines via Pd-catalyzed carboamination reactions: use of allylic strain to control product stereochemistry through N-substituent manipulation.

Authors:  Natalie C Giampietro; John P Wolfe
Journal:  J Am Chem Soc       Date:  2008-09-06       Impact factor: 15.419

3.  Allylation of isatin-derived N-Boc-hydrazones followed by Pd-catalyzed carboamination reaction: an entry to 3-spiro-pyrazolidyl-oxindoles.

Authors:  Stefano Gazzotti; Marco Manenti; Leonardo Lo Presti; Alessandra Silvani
Journal:  RSC Adv       Date:  2019-11-20       Impact factor: 4.036

4.  LFZ-4-46, a tetrahydroisoquinoline derivative, induces apoptosis and cell cycle arrest via induction of DNA damage and activation of MAPKs pathway in cancer cells.

Authors:  Lili Xu; Guozheng Huang; Zhihui Zhu; Shasha Tian; Yingying Wei; Huanwu Hong; Xiaowei Lu; Ying Li; Feize Liu; Huajun Zhao
Journal:  Anticancer Drugs       Date:  2021-09-01       Impact factor: 2.248

  4 in total

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