Literature DB >> 19447036

Design and synthesis of 3-alkyl-2-aryl-1,3-thiazinan-4-one derivatives as selective cyclooxygenase (COX-2) inhibitors.

Tannaz Zebardast1, Afshin Zarghi, Bahram Daraie, Mehdi Hedayati, Orkideh G Dadrass.   

Abstract

A new group of 3-alkyl-2-aryl-1,3-thiazinan-4-ones, possessing a methylsulfonyl pharmacophore, were synthesized and their biological activities were evaluated for cyclooxygenase-2 (COX-2) inhibitory activity. In vitro COX-1/COX-2 inhibition studies identified 3-benzyl-2-(4-methylsulfonylphenyl)-1,3-thiazinan-4-one (11a) as a potent (IC(50)=0.06 microM) and selective (selectivity index >285) COX-2 inhibitor.

Entities:  

Mesh：

Substances：

Year:  2009        PMID： 19447036     DOI： 10.1016/j.bmcl.2009.04.125

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


  8 in total

1.  Synthesis of unsymmetrical 3,4-diaryl-3-pyrrolin-2-ones utilizing pyrrole Weinreb amides.

Authors:  Jessica G Greger; Sarah J P Yoon-Miller; Nathan R Bechtold; Scott A Flewelling; Jacob P MacDonald; Catherine R Downey; Eric A Cohen; Erin T Pelkey
Journal:  J Org Chem       Date:  2011-09-26       Impact factor: 4.354

2.  Convenient diastereoselective synthesis of annulated 3-substituted-(5S*,6S*,Z)-2-(2-(2,4-dinitrophenyl)hydrazono)-5,6-diphenyl-1,3-thiazinan-4-ones.

Authors:  Alaa A Hassan; Nasr K Mohamed; Ashraf A Aly; Hendawy N Tawfeek; Henning Hopf; Stefan Bräse; Martin Nieger
Journal:  Mol Divers       Date:  2019-01-03       Impact factor: 2.943

3.  Modeling the binding modes of stilbene analogs to cyclooxygenase-2: a molecular docking study.

Authors:  Souhila Bouaziz-Terrachet; Amel Toumi-Maouche; Boubekeur Maouche; Safia Taïri-Kellou
Journal:  J Mol Model       Date:  2010-03-17       Impact factor: 1.810

4.  Discovery of new non-acidic lonazolac analogues with COX-2 selectivity as potent anti-inflammatory agents.

Authors:  Marwa F Harras; Rehab Sabour; Omkulthom Mohamed Alkamali
Journal:  Medchemcomm       Date:  2019-07-22       Impact factor: 3.597

5.  Selective COX-2 Inhibitors: A Review of Their Structure-Activity Relationships.

Authors:  Afshin Zarghi; Sara Arfaei
Journal:  Iran J Pharm Res       Date:  2011       Impact factor: 1.696

Review 6.  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

7.  Dihydropyrazole Derivatives Containing Benzo Oxygen Heterocycle and Sulfonamide Moieties Selectively and Potently Inhibit COX-2: Design, Synthesis, and Anti-Colon Cancer Activity Evaluation.

Authors:  Xiao-Qiang Yan; Zhong-Chang Wang; Bo Zhang; Peng-Fei Qi; Gui-Gen Li; Hai-Liang Zhu
Journal:  Molecules       Date:  2019-04-30       Impact factor: 4.411

8.  Synthesis, 3D-QSAR, and Molecular Modeling Studies of Triazole Bearing Compounds as a Promising Scaffold for Cyclooxygenase-2 Inhibition.

Authors:  Ranza Elrayess; Mohamed Saleh Elgawish; Marwa Elewa; Mohamed S Nafie; Sameh S Elhady; Asmaa S A Yassen
Journal:  Pharmaceuticals (Basel)       Date:  2020-11-06
  8 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.