Literature DB >> 4009611

Antiulcer agents. 1. Gastric antisecretory and cytoprotective properties of substituted imidazo[1,2-a]pyridines.

J J Kaminski, J A Bristol, C Puchalski, R G Lovey, A J Elliott, H Guzik, D M Solomon, D J Conn, M S Domalski, S C Wong.   

Abstract

A novel class of antiulcer agents, the substituted imidazo[1,2-a]pyridines, is described. The present compounds are not histamine (H2) receptor antagonists nor are they prostaglandin analogues, yet they exhibit both gastric antisecretory and cytoprotective properties. The mechanism of gastric antisecretory activity may involve inhibition of the H+/K+-ATPase enzyme. Structure-activity studies led to the identification of 3-(cyanomethyl)-2-methyl-8-(phenylmethoxy)imidazo[1,2-a]pyridine, SCH 28080 (27), which was selected for further development and clinical evaluation.

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Year:  1985        PMID: 4009611     DOI: 10.1021/jm00145a006

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


  7 in total

Review 1.  Molecular mechanisms in therapy of acid-related diseases.

Authors:  J M Shin; O Vagin; K Munson; M Kidd; I M Modlin; G Sachs
Journal:  Cell Mol Life Sci       Date:  2008-01       Impact factor: 9.261

2.  Ι₂-mediated amination/cyclization of ketones with 2-aminopyridines under high-speed ball milling: solvent- and metal-free synthesis of 2,3-substituted imidazo[1,2-a]pyridines and zolimidine.

Authors:  Fang-Jian Wang; Hui Xu; Ming Xin; Ze Zhang
Journal:  Mol Divers       Date:  2016-03-14       Impact factor: 2.943

Review 3.  The gastric HK-ATPase: structure, function, and inhibition.

Authors:  Jai Moo Shin; Keith Munson; Olga Vagin; George Sachs
Journal:  Pflugers Arch       Date:  2008-06-06       Impact factor: 3.657

Review 4.  Pharmacological aspects of acid secretion.

Authors:  B I Hirschowitz; D Keeling; M Lewin; S Okabe; M Parsons; K Sewing; B Wallmark; G Sachs
Journal:  Dig Dis Sci       Date:  1995-02       Impact factor: 3.199

5.  The cryo-EM structure of gastric H+,K+-ATPase with bound BYK99, a high-affinity member of K+-competitive, imidazo[1,2-a]pyridine inhibitors.

Authors:  Kazuhiro Abe; Jun Shimokawa; Mao Naito; Keith Munson; Olga Vagin; George Sachs; Hiroshi Suzuki; Kazutoshi Tani; Yoshinori Fujiyoshi
Journal:  Sci Rep       Date:  2017-07-26       Impact factor: 4.379

6.  Discovery and Optimization of Novel 5-Indolyl-7-arylimidazo[1,2-a]pyridine-8-carbonitrile Derivatives as Potent Antitubulin Agents Targeting Colchicine-binding Site.

Authors:  Xin Zhai; Xiaoqiang Wang; Jiao Wang; Jin Liu; Daiying Zuo; Nan Jiang; Tianfang Zeng; Xiuxiu Yang; Tongfei Jing; Ping Gong
Journal:  Sci Rep       Date:  2017-02-27       Impact factor: 4.379

7.  Synthesis, biological evaluation and molecular docking studies of 6-(4-nitrophenoxy)-1H-imidazo[4,5-b]pyridine derivatives as novel antitubercular agents: future DprE1 inhibitors.

Authors:  Jineetkumar Gawad; Chandrakant Bonde
Journal:  Chem Cent J       Date:  2018-12-19       Impact factor: 4.215

  7 in total

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