Abstract
In this paper we report the synthesis and the inhibition on Human Leucocyte Elastase (HLE) of a new series of thieno[2,3-d][1,3]oxazin- or thioxazin-4-ones 3a-o and thieno[3,2-d][1,3]oxazin- or thioxazin-4-ones 6a-d. New derivatives have inhibitory activity in the micromolar range and among them, 2-(3- trifluoromethylphenylamino)-4H-thieno[2,3-d][1,3]oxazin-4-one 3h and 5,6-dimethyl-2-(4-nitrophenylamino)- 4H-thieno[2,3-d][1,3]thioxazin-4-one 3o were the most interesting.
Keywords: Human leucocyte elastase, HLE, Pulmonary diseases, Thienoxazin-4-ones, Thienothioxazin-4-ones
Letters in Drug Design & Discovery
Title: Inhibition of Human Leucocyte Elastase by Novel Thieno-1,3-oxazin-4-ones and Thieno-1,3-thioxazin-4-ones
Volume: 4 Issue: 6
Author(s): N.A. Santagati, L. Salerno, C. Di Giacomo, L. Vanella and S. Ronsisvalle
Affiliation:
Keywords: Human leucocyte elastase, HLE, Pulmonary diseases, Thienoxazin-4-ones, Thienothioxazin-4-ones
Abstract: In this paper we report the synthesis and the inhibition on Human Leucocyte Elastase (HLE) of a new series of thieno[2,3-d][1,3]oxazin- or thioxazin-4-ones 3a-o and thieno[3,2-d][1,3]oxazin- or thioxazin-4-ones 6a-d. New derivatives have inhibitory activity in the micromolar range and among them, 2-(3- trifluoromethylphenylamino)-4H-thieno[2,3-d][1,3]oxazin-4-one 3h and 5,6-dimethyl-2-(4-nitrophenylamino)- 4H-thieno[2,3-d][1,3]thioxazin-4-one 3o were the most interesting.
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N.A. Santagati , L. Salerno , C. Di Giacomo , L. Vanella and S. Ronsisvalle , Inhibition of Human Leucocyte Elastase by Novel Thieno-1,3-oxazin-4-ones and Thieno-1,3-thioxazin-4-ones, Letters in Drug Design & Discovery 2007; 4 (6) . https://dx.doi.org/10.2174/157018007781387764
DOI https://dx.doi.org/10.2174/157018007781387764 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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