Literature DB >> 17531479

2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 2: orally bioavailable compounds.

Hiroyuki Kai1, Yasuhide Morioka, Minoru Tomida, Tadashi Takahashi, Maki Hattori, Kohji Hanasaki, Katsumi Koike, Hiroki Chiba, Shunji Shinohara, Toshiyuki Kanemasa, Yuka Iwamoto, Kohji Takahashi, Yoshitaka Yamaguchi, Takahiko Baba, Takayoshi Yoshikawa, Hideyuki Takenaka.   

Abstract

Structure-activity relationships and efforts to optimize the pharmacokinetic profile of a class of 2-arylimino-5,6-dihydro-4H-1,3-thiazines as cannabinoid receptor agonists are described. Among the compounds examined, compound 14 showed potent affinity and high selectivity for CB2, and compound 23 showed potent affinities against CB1 and CB2. These compounds displayed oral bioavailability.

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Year:  2007        PMID: 17531479     DOI: 10.1016/j.bmcl.2007.04.099

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


  3 in total

1.  Synthesis and Transformation of (-)-Isopulegol-Based Chiral β-Aminolactones and β-Aminoamides.

Authors:  Tam Minh Le; Péter Bérdi; István Zupkó; Ferenc Fülöp; Zsolt Szakonyi
Journal:  Int J Mol Sci       Date:  2018-11-08       Impact factor: 5.923

2.  Discovery of Oxazol-2-amine Derivatives as Potent Novel FLT3 Inhibitors.

Authors:  Hyo Jeong Kim; Hwani Ryu; Jie-Young Song; Sang-Gu Hwang; Shivakumar S Jalde; Hyun-Kyung Choi; Jiyeon Ahn
Journal:  Molecules       Date:  2020-11-05       Impact factor: 4.411

Review 3.  Chemistry of Substituted Thiazinanes and Their Derivatives.

Authors:  Alaa A Hassan; Stefan Bräse; Ashraf A Aly; Hendawy N Tawfeek
Journal:  Molecules       Date:  2020-11-28       Impact factor: 4.411

  3 in total

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