Literature DB >> 19596198

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

Afshin Zarghi1, Tannaz Zebardast, Bahram Daraie, Mehdi Hedayati.   

Abstract

A new group of 1, 3-benthiazinan-4-ones, possessing a methyl sulfonyl 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-(p-fluoropheny)-2-(4-methylsulfonylphenyl)-1,3-benzthiazinan-4-one (7b) as a potent (IC(50)=0.05 microM) and selective (selectivity index=259) COX-2 inhibitor.

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Year:  2009        PMID： 19596198     DOI： 10.1016/j.bmc.2009.06.056

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  11 in total

1.  Pharmacophore elucidation and molecular docking studies on 5-phenyl-1-(3-pyridyl)-1h-1,2,4-triazole-3-carboxylic acid derivatives as COX-2 inhibitors.

Authors:  Marc Lindner; Wolfgang Sippl; Awwad A Radwan
Journal:  Sci Pharm       Date:  2010-03-19

2.  2-(3-Nitro-phen-yl)-3-phenyl-2,3-di-hydro-4H-1,3-benzo-thia-zin-4-one.

Authors:  Hemant P Yennawar; Lee J Silverberg; Michael J Minehan; John Tierney
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-10-23

3.  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

4.  Crystal structure of 2,3-diphenyl-2,3-di-hydro-4H-1,3-benzo-thia-zin-4-one 1-oxide.

Authors:  Hemant P Yennawar; Ryan Fox; Quentin J Moyer; Ziwei Yang; Lee J Silverberg
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2017-07-17

5.  Crystallography, Molecular Modeling, and COX-2 Inhibition Studies on Indolizine Derivatives.

Authors:  Katharigatta N Venugopala; Sandeep Chandrashekharappa; Christophe Tratrat; Pran Kishore Deb; Rahul D Nagdeve; Susanta K Nayak; Mohamed A Morsy; Pobitra Borah; Fawzi M Mahomoodally; Raghu Prasad Mailavaram; Mahesh Attimarad; Bandar E Aldhubiab; Nagaraja Sreeharsha; Anroop B Nair; Osama I Alwassil; Michelyne Haroun; Viresh Mohanlall; Pottathil Shinu; Rashmi Venugopala; Mahmoud Kandeel; Belakatte P Nandeshwarappa; Yasmine F Ibrahim
Journal:  Molecules       Date:  2021-06-10       Impact factor: 4.411

6.  2,3-Diphenyl-2,3-di-hydro-4H-1,3-benzo-thia-zin-4-one.

Authors:  Hemant P Yennawar; Ryan V Bendinsky; David J Coyle; Aaron S Cali; Lee J Silverberg
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2014-03-22

7.  QSAR Modeling of COX -2 Inhibitory Activity of Some Dihydropyridine and Hydroquinoline Derivatives Using Multiple Linear Regression (MLR) Method.

Authors:  Somaye Akbari; Tannaz Zebardast; Afshin Zarghi; Zahra Hajimahdi
Journal:  Iran J Pharm Res       Date:  2017       Impact factor: 1.696

8.  Crystal structures of two 2,3-diaryl-2,3-di-hydro-4H-1,3-benzo-thia-zin-4-ones.

Authors:  Hemant P Yennawar; Michaela J Buchwalter; Baylee K Colburn; Lee J Silverberg
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2018-02-20

9.  Synthesis and biological evaluation of benzothiazin-4-ones: a possible new class of acetylcholinesterase inhibitors.

Authors:  Gabriele A Berwaldt; Daniela P Gouvêa; Daniel S da Silva; Adriana M das Neves; Mayara S P Soares; Juliana H Azambuja; Geonir M Siqueira; Roselia M Spanevello; Wilson Cunico
Journal:  J Enzyme Inhib Med Chem       Date:  2019-12       Impact factor: 5.051

10.  Novel Series of Methyl 3-(Substituted Benzoyl)-7-Substituted-2-Phenylindolizine-1-Carboxylates as Promising Anti-Inflammatory Agents: Molecular Modeling Studies.

Authors:  Katharigatta N Venugopala; Omar H A Al-Attraqchi; Christophe Tratrat; Susanta K Nayak; Mohamed A Morsy; Bandar E Aldhubiab; Mahesh Attimarad; Anroop B Nair; Nagaraja Sreeharsha; Rashmi Venugopala; Michelyne Haroun; Meravanige B Girish; Sandeep Chandrashekharappa; Osama I Alwassil; Bharti Odhav
Journal:  Biomolecules       Date:  2019-10-28
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