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Synthesis and evaluation of pseudosaccharin amine derivates as potential elastase inhibitors / von Rode Haridas Baburao

Pseudosaccharin amines, Heterocycles, Elastase inhibitions, Reversible inhibitions, molecular modelling

PPN (Catalogue-ID): 509329357
Personen: Baburao, Rode Haridas
Format: eBook eBook
Language: English
Published: 2005
Hochschule: Greifswald, Univ., Diss., 2006
Basisklassifikation: 44.42
35.74
Subjects:

Enzyminhibitor

Formangabe: Hochschulschrift
Physical Description: Online-Ressource (PDF-Datei: 154 S., 1880 KB)
Technische Details: Systemvoraussetzungen: Acrobat reader.

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520 |a Elastase is a serine protease which by definition is able to solubilize elastin by hydrolytic cleavage.Human Leukocyte Elastase, HLE (EC 3.4.21.37), is involved in deseases such as adult respiatory distress syndrome, pulmonary emphysema, smoking related chronic bronchitits, ischemic-reperfusion injury and rheumatoid arthritis. Hence, the elastase inhibitors have clinical utility in these diseases. Heterocyclic compounds are one of the most important classes of the elastase inhibitiors. In the present work different pseudosaccharin amine derivatives were synthesized and tested against the elastase. The synthesis of pseudosaccharin amine dervatives was carried out from the amines and(1,1-dioxobenzo[d]isothiazol-3-ylsulfanyl)acetonitrile in different solvents. Futhermore, the pseudosaccharin amines were obtained by refluxing the thiosaccarinates in absolute acetic acid. The reaction of 3-ethoxybenzo[d]isothiazole 1,1-dioxide with different amines in dioxane under reflux resulted into the desired pseudosaccharin amine derivatives in higher yields. Pseudosaccharin chloride was also used in the synthesis of these derivatives ... 
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