Literature DB >> 28328173

Design, synthesis, biological evaluation, and molecular docking of novel flavones as H3 R inhibitors.

Gang Wen1, Qian Liu1, Huabin Hu1, Dongmei Wang1, Song Wu1.   

Abstract

A series of novel flavone derivatives were designed, synthesized, and evaluated for their H3 R inhibitory activity. The results showed that four compounds exhibited significant anti-H3 R activity. Molecular docking experiments indicated that a salt bridge, hydrogen-bonding, and hydrophobic interactions all contributed to interactions between inhibitors and H3 R.
© 2017 John Wiley & Sons A/S.

Entities:  

Keywords:  H3R inhibitor; crystal structure; flavone; homology modeling; molecular docking

Mesh:

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Year:  2017        PMID: 28328173     DOI: 10.1111/cbdd.12981

Source DB:  PubMed          Journal:  Chem Biol Drug Des        ISSN: 1747-0277            Impact factor:   2.817


  2 in total

1.  Flavonoids enhance rod opsin stability, folding, and self-association by directly binding to ligand-free opsin and modulating its conformation.

Authors:  Joseph T Ortega; Tanu Parmar; Beata Jastrzebska
Journal:  J Biol Chem       Date:  2019-04-03       Impact factor: 5.157

2.  Design, synthesis, and biological evaluation of novel iso-flavones derivatives as H3R antagonists.

Authors:  Jian Xin; Min Hu; Qian Liu; Tian Tai Zhang; Dong Mei Wang; Song Wu
Journal:  J Enzyme Inhib Med Chem       Date:  2018-12       Impact factor: 5.051

  2 in total

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