Phosphonates and Phosphinates: Novel Leaving Groups for Benzisothiazolone Inhibitors of Human Leukocyte Elastase
โ Scribed by Desai, Ranjit C.; Court, John C.; Ferguson, Edward; Gordon, Robert J.; Hlasta, Dennis J.; Dunlap, Richard P.; Franke, Catherine A.
- Book ID
- 127305492
- Publisher
- American Chemical Society
- Year
- 1995
- Tongue
- English
- Weight
- 422 KB
- Volume
- 38
- Category
- Article
- ISSN
- 0022-2623
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๐ SIMILAR VOLUMES
The [ 4C] labelled synthesis of two benzisothiazolone based inhibitors of Human Leukocyte Elastase is described. These are The synthesis of the intermediate [3-14C]-2-(chloromethyl)-6-methoxy-4-( l-methylethyl)-l,2benzisothiazol-3(2H)-one 1 ,I-dioxide, 8, common to both these syntheses. was achieve
Distinct differences in the SAR for HLE and PPE inhibition in this class of compounds were observed. For example, larger lipophilic substituents at the benzisothiazolone 4-position afforded inhibitors that were potent against HLE, but inactive against PPE. These findings are consistent with computer