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Literature DB >> 21696952

Pyrazole-based sulfonamide and sulfamides as potent inhibitors of mammalian 15-lipoxygenase.

Khehyong Ngu¹, David S Weinstein, Wen Liu, Charles Langevine, Donald W Combs, Shaobin Zhuang, Xing Chen, Cort S Madsen, Timothy W Harper, Saleem Ahmad, Jeffrey A Robl.

Abstract

A series of inhibitors of mammalian 15-lipoxygenase (15-LO) based on a 3,4,5-tri-substituted pyrazole scaffold is described. Replacement of a sulfonamide functionality in the lead series with a sulfamide group resulted in improved physicochemical properties generating analogs with enhanced inhibition in cell-based and whole blood assays.

Entities: Chemical Gene Species

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Year: 2011 PMID： 21696952 DOI： 10.1016/j.bmcl.2011.05.107

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

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Cited

10 in total

1. 15-Lipoxygenase inhibition of Commelina benghalensis, Tradescantia fluminensis, Tradescantia zebrina.

Authors: Cean Socorro M Alaba; Christine L Chichioco-Hernandez
Journal: Asian Pac J Trop Biomed Date: 2014-03

2. Human 15-LOX-1 active site mutations alter inhibitor binding and decrease potency.

Authors: Michelle Armstrong; Christopher van Hoorebeke; Thomas Horn; Joshua Deschamps; J Cody Freedman; Chakrapani Kalyanaraman; Matthew P Jacobson; Theodore Holman
Journal: Bioorg Med Chem Date: 2016-08-31 Impact factor: 3.641

3. 4-Chlorophenyl-N-furfuryl-1,2,4-triazole Methylacetamides as Significant 15-Lipoxygenase Inhibitors: an Efficient Approach for Finding Lead Anti-inflammatory Compounds.

Authors: Muhammad Yasin; Wardah Shahid; Muhammad Ashraf; Muhammad Saleem; Saima Muzaffar; Syed Abid Ejaz; Amna Saeed; Thomas Majer; Keshab Bhattarai; Naheed Riaz
Journal: ACS Omega Date: 2022-05-31

4. The potential of 12/15-lipoxygenase inhibitors in stroke therapy.

Authors: Klaus van Leyen; Theodore R Holman; David J Maloney
Journal: Future Med Chem Date: 2014 Impact factor: 3.808

5. Potent and selective inhibitors of human reticulocyte 12/15-lipoxygenase as anti-stroke therapies.

Authors: Ganesha Rai; Netra Joshi; Joo Eun Jung; Yu Liu; Lena Schultz; Adam Yasgar; Steve Perry; Giovanni Diaz; Qiangli Zhang; Victor Kenyon; Ajit Jadhav; Anton Simeonov; Eng H Lo; Klaus van Leyen; David J Maloney; Theodore R Holman
Journal: J Med Chem Date: 2014-05-13 Impact factor: 7.446

Pyrazole-based sulfonamide and sulfamides as potent inhibitors of mammalian 15-lipoxygenase.

1. 15-Lipoxygenase inhibition of Commelina benghalensis, Tradescantia fluminensis, Tradescantia zebrina.

2. Human 15-LOX-1 active site mutations alter inhibitor binding and decrease potency.

3. 4-Chlorophenyl-N-furfuryl-1,2,4-triazole Methylacetamides as Significant 15-Lipoxygenase Inhibitors: an Efficient Approach for Finding Lead Anti-inflammatory Compounds.

4. The potential of 12/15-lipoxygenase inhibitors in stroke therapy.

5. Potent and selective inhibitors of human reticulocyte 12/15-lipoxygenase as anti-stroke therapies.

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

Review 7. Fatty Acid Allosteric Regulation of C-H Activation in Plant and Animal Lipoxygenases.

8. Activity-Based Probes for 15-Lipoxygenase-1.

9. Visible light-promoted ring-opening functionalization of unstrained cycloalkanols via inert C-C bond scission.

10. Rational Development of a Potent 15-Lipoxygenase-1 Inhibitor with in Vitro and ex Vivo Anti-inflammatory Properties.