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Literature DB >> 20638756

Inhibitors of human neutrophil elastase based on a highly functionalized N-amino-4-imidazolidinone scaffold.

Guijia He¹, Dengfeng Dou, Liuqing Wei, Kevin R Alliston, William C Groutas.

Abstract

A series of compounds based on the N-amino-4-imidazolidinone scaffold was synthesized and screened against human neutrophil elastase (HNE). These studies lead to the identification of a selective, low micromolar reversible competitive inhibitor of HNE. 2010 Elsevier Masson SAS. All rights reserved.

Entities: CellLine Chemical Disease Gene Species

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Year: 2010 PMID： 20638756 PMCID： PMC2918731 DOI： 10.1016/j.ejmech.2010.06.028

Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514

38 in total

1. Noncovalent inhibitors of human leukocyte elastase based on the 4-imidazolidinone scaffold.

Authors: Liuqing Wei; Xiangdong Gan; Jiaying Zhong; Kevin R Alliston; William C Groutas
Journal: Bioorg Med Chem Date: 2003-11-17 Impact factor: 3.641

2. The determination of enzyme inhibitor constants.

Authors: M DIXON
Journal: Biochem J Date: 1953-08 Impact factor: 3.857

Review 3. The pathogenesis of chronic obstructive pulmonary disease: advances in the past 100 years.

Authors: Steven D Shapiro; Edward P Ingenito
Journal: Am J Respir Cell Mol Biol Date: 2005-05 Impact factor: 6.914

Review 4. Neutrophil serine proteases: specific regulators of inflammation.

Authors: Christine T N Pham
Journal: Nat Rev Immunol Date: 2006-07 Impact factor: 53.106

Review 5. Neutrophil elastase, proteinase 3 and cathepsin G: physicochemical properties, activity and physiopathological functions.

Authors: Brice Korkmaz; Thierry Moreau; Francis Gauthier
Journal: Biochimie Date: 2007-10-25 Impact factor: 4.079

6. Cigarette smoke-induced emphysema in A/J mice is associated with pulmonary oxidative stress, apoptosis of lung cells, and global alterations in gene expression.

Authors: Tirumalai Rangasamy; Vikas Misra; Lijie Zhen; Clarke G Tankersley; Rubin M Tuder; Shyam Biswal
Journal: Am J Physiol Lung Cell Mol Physiol Date: 2009-03-13 Impact factor: 5.464

Review 1. Neutrophil elastase inhibitors.

Authors: William C Groutas; Dengfeng Dou; Kevin R Alliston
Journal: Expert Opin Ther Pat Date: 2011-01-16 Impact factor: 6.674

1 in total

Inhibitors of human neutrophil elastase based on a highly functionalized N-amino-4-imidazolidinone scaffold.

1. Noncovalent inhibitors of human leukocyte elastase based on the 4-imidazolidinone scaffold.

2. The determination of enzyme inhibitor constants.

Review 3. The pathogenesis of chronic obstructive pulmonary disease: advances in the past 100 years.

Review 4. Neutrophil serine proteases: specific regulators of inflammation.

Review 5. Neutrophil elastase, proteinase 3 and cathepsin G: physicochemical properties, activity and physiopathological functions.

6. Cigarette smoke-induced emphysema in A/J mice is associated with pulmonary oxidative stress, apoptosis of lung cells, and global alterations in gene expression.

7. On the size of the active site in proteases. I. Papain.

Review 8. Mediators of chronic obstructive pulmonary disease.

9. Mechanism-based inhibitors of serine proteases with high selectivity through optimization of S' subsite binding.

Review 10. Testing drugs in animal models of cigarette smoke-induced chronic obstructive pulmonary disease.

Review 1. Neutrophil elastase inhibitors.