Literature DB >> 20488702

Synthesis and biological evaluation of azobicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes.

Tang Peng Cho1, Yang Fang Long, Lin Zhi Gang, Wang Yang, Lu He Jun, Shen Guang Yuan, Fu Jian Hong, Wang Lin, Guan Dong Liang, Zhang Lei, Luo Jing Jing, Gong Ai Shen, She Gao Hong, Wang Dan, Feng Ying, Yan Pang Ke, Leng Ying, Feng Jun, Mong Xian Tai.   

Abstract

A series of novel azobicyclo[3.3.0]octane derivatives were synthesized and evaluated as dipeptidyl peptidase 4 (DPP-4) inhibitors. The effort resulted in the discovery of inhibitor 2a, which exhibited excellent efficacies in an oral glucose tolerance test. Introduction of methyl group (2j) could prolong the inhibition of serum DPP-4 activity. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20488702     DOI: 10.1016/j.bmcl.2010.04.120

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


  2 in total

1.  Discovery of VU6028418: A Highly Selective and Orally Bioavailable M4 Muscarinic Acetylcholine Receptor Antagonist.

Authors:  Matthew Spock; Trever R Carter; Katrina A Bollinger; Changho Han; Logan A Baker; Alice L Rodriguez; Li Peng; Jonathan W Dickerson; Aidong Qi; Jerri M Rook; Jordan C O'Neill; Katherine J Watson; Sichen Chang; Thomas M Bridges; Julie L Engers; Darren W Engers; Colleen M Niswender; P Jeffrey Conn; Craig W Lindsley; Aaron M Bender
Journal:  ACS Med Chem Lett       Date:  2021-08-02       Impact factor: 4.632

2.  Discovery of the First Selective M4 Muscarinic Acetylcholine Receptor Antagonists with in Vivo Antiparkinsonian and Antidystonic Efficacy.

Authors:  Mark S Moehle; Aaron M Bender; Jonathan W Dickerson; Daniel J Foster; Aidong Qi; Hyekyung P Cho; Yuping Donsante; Weimin Peng; Zoey Bryant; Kaylee J Stillwell; Thomas M Bridges; Sichen Chang; Katherine J Watson; Jordan C O'Neill; Julie L Engers; Li Peng; Alice L Rodriguez; Colleen M Niswender; Craig W Lindsley; Ellen J Hess; P Jeffrey Conn; Jerri M Rook
Journal:  ACS Pharmacol Transl Sci       Date:  2021-08-02
  2 in total

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