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[14C]-labelling of benzisothiazolone based inhibitors of human leukocyte elastase

โœ Scribed by Alain Burgos; Gordon R. Duffin; George J. Ellames; Karen J. Wedge

Publisher
John Wiley and Sons
Year
1996
Tongue
French
Weight
418 KB
Volume
38
Category
Article
ISSN
0022-2135

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โœฆ Synopsis

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 achieved in 8 steps in 37% radiochemical yield.

๐Ÿ“œ SIMILAR VOLUMES

A comparative SAR and computer modeling
A comparative SAR and computer modeling study of benzisothiazolone, mechanism-based inhibitors with porcine pancreatic and human leukocyte elastase
โœ Dennis J. Hlasta; John J. Court; Ranjit C. Desai; Timothy G. Talomie; Jian Shen; ๐Ÿ“‚ Article ๐Ÿ“… 1996 ๐Ÿ› Elsevier Science ๐ŸŒ English โš– 332 KB

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