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Letters in Drug Design & Discovery

Author(s): N.A. Santagati, L. Salerno, C. Di Giacomo, L. Vanella and S. Ronsisvalle

DOI: 10.2174/157018007781387764

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Inhibition of Human Leucocyte Elastase by Novel Thieno-1,3-oxazin-4-ones and Thieno-1,3-thioxazin-4-ones

Page: [386 - 393] Pages: 8

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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