Literature DB >> 18440813

The SAR studies of novel CB2 selective agonists, benzimidazolone derivatives.

Hirofumi Omura1, Makoto Kawai, Akiko Shima, Yasuhiro Iwata, Fumitaka Ito, Tsutomu Masuda, Atsuko Ohta, Naoya Makita, Kiyoyuki Omoto, Hiromi Sugimoto, Akira Kikuchi, Hiroshi Iwata, Kazuo Ando.   

Abstract

Benzimidazolone derivatives were discovered as novel CB2 selective agonists. Structure Activity Relationship (SAR) studies around them were examined to improve metabolic stability. Compound 39 exhibited excellent metabolic stability in human liver microsomes (HLM) and significant attenuation of the chronic colonic allodynia in the TNBS-treated rats by po administration.

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Year:  2008        PMID： 18440813     DOI： 10.1016/j.bmcl.2008.04.032

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


  4 in total

1.  Diversity oriented synthesis and IKK inhibition of aminobenzimidazole tethered quinazoline-2,4-diones, thioxoquinazolin-4-ones, benzodiazepine-2,3,5-triones, isoxazoles and isoxazolines.

Authors:  Sureshbabu Dadiboyena; Aïcha Arfaoui; Hassen Amri; F Javier Piedrafita; Adel Nefzi
Journal:  Bioorg Med Chem Lett       Date:  2014-12-08       Impact factor: 2.823

2.  Construction of a bicyclic beta-benzyloxy and beta-hydroxy amide library through a multicomponent cyclization reaction.

Authors:  Li Zhang; Qing Xiao; Chao Ma; Xiang-Qun Xie; Paul E Floreancig
Journal:  J Comb Chem       Date:  2009 Jul-Aug

3.  Synthesis and antibacterial activities of 1-alkyl-3-methacryloyl (acryloyl) of benzimidazolone (thione) derivatives.

Authors:  Shaopeng Wei; Wenjun Wu; Zhiqin Ji
Journal:  Int J Mol Sci       Date:  2012-04-16       Impact factor: 6.208

4.  Route to Benzimidazol-2-ones via Decarbonylative Ring Contraction of Quinoxalinediones: Application to the Synthesis of Flibanserin, A Drug for Treating Hypoactive Sexual Desire Disorder in Women and Marine Natural Product Hunanamycin Analogue.

Authors:  Rahul D Shingare; Akshay S Kulkarni; Revannath L Sutar; D Srinivasa Reddy
Journal:  ACS Omega       Date:  2017-08-29
  4 in total

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