Literature DB >> 18707091

Effect of cathepsin K inhibitors on bone resorption.

Naoki Teno1, Keiichi Masuya, Takeru Ehara, Takatoshi Kosaka, Takahiro Miyake, Osamu Irie, Yuko Hitomi, Naoko Matsuura, Ichiro Umemura, Genji Iwasaki, Hiroaki Fukaya, Kazuhiro Toriyama, Noriko Uchiyama, Kazuhiko Nonomura, Ikuo Sugiyama, Motohiko Kometani.   

Abstract

On the basis of the pyrrolopyrimidine core structure that was previously discovered, cathepsin K inhibitors having a spiro amine at the P3 have been explored to enhance the target, bone marrow, tissue distribution. Several spiro structures were identified with improved distribution toward bone marrow. The representative inhibitor 7 of this series revealed in vivo reduction in C-terminal telopeptide of type I collagen in rats and monkeys.

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Year:  2008        PMID: 18707091     DOI: 10.1021/jm800626a

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  5 in total

1.  Discovery of 3,3'-Spiro[Azetidine]-2-oxo-indoline Derivatives as Fusion Inhibitors for Treatment of RSV Infection.

Authors:  Weihua Shi; Zhigan Jiang; Haiying He; Fubiao Xiao; Fusen Lin; Ya Sun; Lijuan Hou; Liang Shen; Lixia Han; Minggao Zeng; Kunmin Lai; Zhengxian Gu; Xinsheng Chen; Tao Zhao; Li Guo; Chun Yang; Jian Li; Shuhui Chen
Journal:  ACS Med Chem Lett       Date:  2018-01-10       Impact factor: 4.345

2.  Discovery of Orally Active and Nonsteroidal Farnesoid X Receptor (FXR) Antagonist with Propensity for Accumulation and Responsiveness in Ileum.

Authors:  Naoki Teno; Yusuke Iguchi; Keisuke Oda; Yukiko Yamashita; Arisa Masuda; Ko Fujimori; Mizuho Une; Keigo Gohda
Journal:  ACS Med Chem Lett       Date:  2021-02-24       Impact factor: 4.345

3.  Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.

Authors:  Aurélie Mallinger; Simon Crumpler; Mark Pichowicz; Dennis Waalboer; Mark Stubbs; Olajumoke Adeniji-Popoola; Bozena Wood; Elizabeth Smith; Ching Thai; Alan T Henley; Katrin Georgi; William Court; Steve Hobbs; Gary Box; Maria-Jesus Ortiz-Ruiz; Melanie Valenti; Alexis De Haven Brandon; Robert TePoele; Birgitta Leuthner; Paul Workman; Wynne Aherne; Oliver Poeschke; Trevor Dale; Dirk Wienke; Christina Esdar; Felix Rohdich; Florence Raynaud; Paul A Clarke; Suzanne A Eccles; Frank Stieber; Kai Schiemann; Julian Blagg
Journal:  J Med Chem       Date:  2015-02-13       Impact factor: 7.446

Review 4.  Advances in the discovery of cathepsin K inhibitors on bone resorption.

Authors:  Jun Lu; Maolin Wang; Ziyue Wang; Zhongqi Fu; Aiping Lu; Ge Zhang
Journal:  J Enzyme Inhib Med Chem       Date:  2018-12       Impact factor: 5.051

Review 5.  Smart Bioinks for the Printing of Human Tissue Models.

Authors:  Zeina Maan; Nadia Z Masri; Stephanie M Willerth
Journal:  Biomolecules       Date:  2022-01-15
  5 in total

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