by U.S. Dept. of Heath, Education, and Welfare, Public Health Service, National Institutes of Health, National Heart, Lung, and Blood Institute, Division of Lung Diseases in [Bethesda, Md.] .
Written in English
Bibliography: p. 8-9.
|Statement||[prepared under contract by James C. Powers]|
|Series||DHEW publication ; no. (NIH) 76-1090, DHEW publication -- no. (NIH) 76-1090.|
|Contributions||Powers, James C.|
|The Physical Object|
|Pagination||, 9 p. ;|
Edwards PD, Meyer EF, Vijayalakshmi J, Tuthill PA, Andisik DA, Gomes B, Strimpler A () Design, synthesis and kinetic evaluation of a unique class of elastase inhibitors, the peptidyl a-ketobenzoxazoles, and the X-ray crystal structure of the covalent complex between porcine pancreatic elastase and the Ac-Ala-Pro-Valbenzoxazole. Diazaborines as new inhibitors of human neutrophil elastase. ACS Omega 3(7), – ().Crossref, Medline, Google Scholar; 5. Crocetti L, Giovannoni MP, Schepetkin IA et al. Design, synthesis and evaluation of N-benzoylindazole derivatives and analogues as inhibitors of human neutrophil elastase. Bioorg. Med. Chem. 19(15), – Author: Beata Donarska, Krzysztof Z Łączkowski. Synthesis and Pharmacological Evaluation of Indole Derivatives as Deaza Analogues of Potent Human Neutrophil Elastase Inhibitors. Letizia Crocetti. NEUROFARBA, Sezione di Farmaceutica e Nutraceutica, Università degli Studi di Firenze, Via Ugo Schiff 6, Sesto Fiorentino, Italy. Ahp-Cyclodepsipeptide Inhibitors of Elastase: Lyngbyastatin 7 Stability, Scalable Synthesis, and Focused Library Analysis ACS Med Chem Lett. Mar 4;11(4) doi: /acsmedchemlett.9b eCollection Apr 9. Authors Danmeng Luo 1.
Abstract. We have recently described the inhibition of human neutrophil elastase (HNE) by RNA purified from Streptococcus pneumoniae (1). Inhibition of this enzyme by a wide variety of polyanions has also been reported by others. Get this from a library! Report of Workshop on Elastase Inhibitors for Treatment of Emphysema Approaches to Synthesis and Biological Evaluation, June , [National Heart, Lung, and Blood Institute. Division of Lung Diseases.;]. Synthesis and in vitro evaluation of pseudosaccharinamine derivatives as potential elastase inhibitors. Bioorganic & Medicinal Chemistry , 14 (8), DOI: / Elastases are a group of serine proteases that specifically degrade elastin. Elastin, together with collagen, is a key protein that contributes to the mechanical properties of connective tissue. There are two types of elastases; pancreatic elastase (E.C. ) and leukocyte elastase (also known as neutrophil elastase) (E.C. ).
Multicomponent Synthesis of new series of 4H-chromenecarboxylate derivatives.. All synthesized compounds found to be potent elastase inhibitors with much lower IC 50 value i.e ± µM.. Estimated Chemoinformatics properties validates Lipinski rule. Elastase is a proteolytic enzyme that hydrolyzes the peptide bonds of elastin (1, 2). It was puzzling to early investigators that elastase activity could be demonstrated only with difficulty, if at all, in fresh extracts of pancreas or pancreatic juice (3, 4). Elastase also stimulates the synthesis of alpha 1 PI in monocytes from homozygous PiZZ alpha 1 PI-deficient individuals, but has no effect on the rate of secretion; hence, the enzyme mediates an effect on alpha 1 PI that increases the intracellular accumulation of inhibitor and exaggerates the intrinsic defect in secretion of alpha 1 PI that. Without the presence of its natural inhibitor, the elastase in abundance generates tissue lesions, since this enzyme is the main protease released by neutrophils in inflammatory processes. The action of Elastase is related to a series of diseases such as liver failure, rheumatoid arthritis, psoriasis, skin cancer, arteriosclerosis and several.