Literature DB >> 17210254

Design and synthesis of pyrimido[4,5-b][1,4]benzothiazine derivatives, as potent 15-lipoxygenase inhibitors.

M Bakavoli1, M Nikpour, M Rahimizadeh, M R Saberi, H Sadeghian.   

Abstract

A group of 2-substituted pyrimido[4,5-b][1,4]benzothiazines were designed, synthesized, and evaluated as potential inhibitors of 15-lipoxygenase (15-LO). Compounds 4d and 4e showed the best IC50 of 15-LO inhibition (IC50=18 and 34 microM, respectively). All compounds were docked into 15-LO. As a result the sulfur atom was oriented toward the iron atom of the active site of 15-LO. We suggest the interaction of the iron atom is essential for the activity of the inhibitors.

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Year:  2006        PMID： 17210254     DOI： 10.1016/j.bmc.2006.12.022

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


  11 in total

1.  Stylosin and some of its synthetic derivatives induce apoptosis in prostate cancer cells as 15-lipoxygenase enzyme inhibitors.

Authors:  Seyed Navid Goftari; Hamid Sadeghian; Ahmad Reza Bahrami; Fatemeh Maleki; Maryam M Matin
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2019-07-11       Impact factor: 3.000

2.  Discovery of potent and selective inhibitors of human reticulocyte 15-lipoxygenase-1.

Authors:  Ganesha Rai; Victor Kenyon; Ajit Jadhav; Lena Schultz; Michelle Armstrong; J Brian Jameson; Eric Hoobler; William Leister; Anton Simeonov; Theodore R Holman; David J Maloney
Journal:  J Med Chem       Date:  2010-10-28       Impact factor: 7.446

3.  2-(chromon-3-yl)imidazole derivatives as potential antimicrobial agents: synthesis, biological evaluation and molecular docking studies.

Authors:  Shweta Sharma; Vishal Sharma; Gurpreet Singh; Harpreet Kaur; Shubham Srivastava; Mohan Paul S Ishar
Journal:  J Chem Biol       Date:  2016-11-16

4.  Involvement of gap junctions between smooth muscle cells in sustained hypoxic pulmonary vasoconstriction development: a potential role for 15-HETE and 20-HETE.

Authors:  Igor V Kizub; Anand Lakhkar; Vidhi Dhagia; Sachindra R Joshi; Houli Jiang; Michael S Wolin; John R Falck; Sreenivasulu Reddy Koduru; Ramu Errabelli; Elizabeth R Jacobs; Michal L Schwartzman; Sachin A Gupte
Journal:  Am J Physiol Lung Cell Mol Physiol       Date:  2016-02-19       Impact factor: 5.464

5.  Crystal structure of (E)-2-benzyl-idene-4-[(3-phenyl-4,5-di-hydro-isoxazol-5-yl)meth-yl]-2H-benzo[b][1,4]thia-zin-3(4H)-one.

Authors:  Nada Kheira Sebbar; Mohamed Ellouz; El Mokhtar Essassi; Mohamed Saadi; Lahcen El Ammari
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2015-05-23

6.  Convenient synthesis of benzothiazinoisoindol-11-ones and benzoindenothiazin-11-ones, and antimicrobial testing thereof.

Authors:  Satbir Mor; Mohini Khatri
Journal:  Mol Divers       Date:  2022-08-03       Impact factor: 3.364

7.  SAR comparative studies on pyrimido[4,5-b][1,4] benzothiazine derivatives as 15-lipoxygenase inhibitors, using ab initio calculations.

Authors:  Mehdi Bakavoli; Hamid Sadeghian; Zahra Tabatabaei; Elham Rezaei; Mohammad Rahimizadeh; Mohsen Nikpour
Journal:  J Mol Model       Date:  2008-04-19       Impact factor: 1.810

8.  New Insight into the SAR of Pyrimido [4,5-b][1,4] Benzothiazines as 15-lipoxygenase Inhibitors.

Authors:  Nona Pooryaghoobi; Mehdi Bakavoli; Maliheh Alimardani; Tahmineh Bazzazan; Hamid Sadeghian
Journal:  Iran J Basic Med Sci       Date:  2013-06       Impact factor: 2.699

9.  Crystal structure of (Z)-ethyl 2-{5-[(2-benzyl-idene-3-oxo-2,3-di-hydro-benzo[b][1,4]thia-zin-4-yl)meth-yl]-1H-1,2,3-triazol-1-yl}acetate.

Authors:  M Ellouz; N K Sebbar; E M Essassi; Y Ouzidan; J T Mague
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2015-12-06

10.  Computational Analysis of LOX1 Inhibition Identifies Descriptors Responsible for Binding Selectivity.

Authors:  Chrysoula Gousiadou; Irene Kouskoumvekaki
Journal:  ACS Omega       Date:  2018-02-26
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